- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
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Ro-3306
RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
CAS No. 872573-93-8
文献中Selleckの製品使用例（146）
製品安全説明書
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Ro-3306関連製品
シグナル伝達経路
CDK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| human HCT116 cells | Cytotoxic assay | 5 days | Cytotoxicity against human HCT116 cells after 5 days by MTS assay， IC50=3.2 μM | 22326168 | |
| A172 | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50 = 5.9079 μM. | SANGER | ||
| PFSK-1 | Growth inhibition assay | Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50 = 5.86168 μM. | SANGER | ||
| GCT | Growth inhibition assay | Inhibition of human GCT cell growth in a cell viability assay, IC50 = 5.85121 μM. | SANGER | ||
| HGC-27 | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50 = 5.73077 μM. | SANGER | ||
| KP-4 | Growth inhibition assay | Inhibition of human KP-4 cell growth in a cell viability assay, IC50 = 5.69823 μM. | SANGER | ||
| NCI-H1792 | Growth inhibition assay | Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50 = 5.47954 μM. | SANGER | ||
| GAMG | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50 = 5.3715 μM. | SANGER | ||
| NB13 | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 5.32786 μM. | SANGER | ||
| SK-MEL-2 | Growth inhibition assay | Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 5.09632 μM. | SANGER | ||
| YH-13 | Growth inhibition assay | Inhibition of human YH-13 cell growth in a cell viability assay, IC50 = 4.75776 μM. | SANGER | ||
| NCI-H2405 | Growth inhibition assay | Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50 = 4.74493 μM. | SANGER | ||
| NEC8 | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50 = 4.47076 μM. | SANGER | ||
| MN-60 | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 4.37623 μM. | SANGER | ||
| LXF-289 | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50 = 4.2176 μM. | SANGER | ||
| PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 4.10805 μM. | SANGER | ||
| COR-L88 | Growth inhibition assay | Inhibition of human COR-L88 cell growth in a cell viability assay, IC50 = 3.47583 μM. | SANGER | ||
| KOSC-2 | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50 = 3.44662 μM. | SANGER | ||
| LB1047-RCC | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 3.23501 μM. | SANGER | ||
| 8-MG-BA | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50 = 3.14049 μM. | SANGER | ||
| 5637 | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50 = 3.08532 μM. | SANGER | ||
| BPH-1 | Growth inhibition assay | Inhibition of human BPH-1 cell growth in a cell viability assay, IC50 = 2.97455 μM. | SANGER | ||
| UM-UC-3 | Growth inhibition assay | Inhibition of human UM-UC-3 cell growth in a cell viability assay, IC50 = 2.73936 μM. | SANGER | ||
| Hs-578-T | Growth inhibition assay | Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50 = 2.27799 μM. | SANGER | ||
| 639-V | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50 = 2.27537 μM. | SANGER | ||
| A4-Fuk | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 2.05604 μM. | SANGER | ||
| SK-N-DZ | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 2.01876 μM. | SANGER | ||
| ALL-PO | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 1.90813 μM. | SANGER | ||
| U251 | Growth inhibition assay | Inhibition of human U251 cell growth in a cell viability assay, IC50 = 1.63771 μM. | SANGER | ||
| SW1710 | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50 = 1.61408 μM. | SANGER | ||
| T98G | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50 = 1.36812 μM. | SANGER | ||
| PA-1 | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50 = 1.22654 μM. | SANGER | ||
| H4 | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50 = 1.15875 μM. | SANGER | ||
| NCI-SNU-1 | Growth inhibition assay | Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 0.73095 μM. | SANGER | ||
| human SJSA1 cells | Proliferation assay | Antiproliferative activity against human SJSA1 cells, IC50=4.55 μM | 17303421 | ||
| human SW480 cells | Proliferation assay | Antiproliferative activity against human SW480 cells, IC50=2.2 μM | 17303421 | ||
| human RKO cells | Proliferation assay | Antiproliferative activity against human RKO cells, IC50=2 μM | 17303421 | ||
| human HCT116 cells | Proliferation assay | Antiproliferative activity against human HCT116 cells, IC50=1.14 μM | 17303421 | ||
| human MDA435 cells | Proliferation assay | Antiproliferative activity against human MDA435 cells, IC50=1.14 μM | 17303421 | ||
| human H460a cells | Proliferation assay | Antiproliferative activity against human H460a cells, IC50=1.04 μM | 17303421 | ||
| KB-3-1 adenocarcinoma cell line | qHTS assay | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 31515284 | ||
| HO-1-N-1 | Growth inhibition assay | Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50 = 5.95425 μM. | SANGER | ||
| HN | Growth inhibition assay | Inhibition of human HN cell growth in a cell viability assay, IC50 = 5.97097 μM. | SANGER | ||
| IST-MES1 | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50 = 5.97521 μM. | SANGER | ||
| TGW | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay, IC50 = 6.05682 μM. | SANGER | ||
| COR-L23 | Growth inhibition assay | Inhibition of human COR-L23 cell growth in a cell viability assay, IC50 = 6.3735 μM. | SANGER | ||
| D-566MG | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50 = 6.78873 μM. | SANGER | ||
| SKG-IIIa | Growth inhibition assay | Inhibition of human SKG-IIIa cell growth in a cell viability assay, IC50 = 6.85572 μM. | SANGER | ||
| NCI-H446 | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50 = 7.0181 μM. | SANGER | ||
| KYSE-270 | Growth inhibition assay | Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50 = 7.03872 μM. | SANGER | ||
| CAL-39 | Growth inhibition assay | Inhibition of human CAL-39 cell growth in a cell viability assay, IC50 = 7.3524 μM. | SANGER | ||
| IST-SL1 | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50 = 7.43349 μM. | SANGER | ||
| SF539 | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay, IC50 = 7.55197 μM. | SANGER | ||
| TE-1 | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 7.89091 μM. | SANGER | ||
| NB10 | Growth inhibition assay | Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 7.98758 μM. | SANGER | ||
| 8505C | Growth inhibition assay | Inhibition of human 8505C cell growth in a cell viability assay, IC50 = 7.99817 μM. | SANGER | ||
| DB | Growth inhibition assay | Inhibition of human DB cell growth in a cell viability assay, IC50 = 8.01131 μM. | SANGER | ||
| NCI-H28 | Growth inhibition assay | Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50 = 8.59884 μM. | SANGER | ||
| LOXIMVI | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 8.63701 μM. | SANGER | ||
| ME-180 | Growth inhibition assay | Inhibition of human ME-180 cell growth in a cell viability assay, IC50 = 8.80395 μM. | SANGER | ||
| ES3 | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 9.12794 μM. | SANGER | ||
| SK-N-FI | Growth inhibition assay | Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 9.41699 μM. | SANGER | ||
| NBsusSR | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50 = 10.2318 μM. | SANGER | ||
| GI-ME-N | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50 = 10.2783 μM. | SANGER | ||
| A704 | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50 = 10.3318 μM. | SANGER | ||
| HuP-T4 | Growth inhibition assay | Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50 = 10.4271 μM. | SANGER | ||
| A101D | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50 = 11.1574 μM. | SANGER | ||
| MCF7 | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50 = 11.1849 μM. | SANGER | ||
| A549 | Growth inhibition assay | Inhibition of human A549 cell growth in a cell viability assay, IC50 = 11.206 μM. | SANGER | ||
| HD-MY-Z | Growth inhibition assay | Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50 = 11.206 μM. | SANGER | ||
| HCC1395 | Growth inhibition assay | Inhibition of human HCC1395 cell growth in a cell viability assay, IC50 = 11.5596 μM. | SANGER | ||
| SK-NEP-1 | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 11.7332 μM. | SANGER | ||
| HSC-2 | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50 = 11.7842 μM. | SANGER | ||
| HCC1937 | Growth inhibition assay | Inhibition of human HCC1937 cell growth in a cell viability assay, IC50 = 11.8473 μM. | SANGER | ||
| RS4-11 | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 11.8836 μM. | SANGER | ||
| CAL-27 | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50 = 12.1637 μM. | SANGER | ||
| NCI-H23 | Growth inhibition assay | Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50 = 12.4155 μM. | SANGER | ||
| A431 | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50 = 12.7233 μM. | SANGER | ||
| HT-1080 | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50 = 12.7373 μM. | SANGER | ||
| GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 12.7716 μM. | SANGER | ||
| BFTC-909 | Growth inhibition assay | Inhibition of human BFTC-909 cell growth in a cell viability assay, IC50 = 13.1068 μM. | SANGER | ||
| CAL-33 | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50 = 13.6518 μM. | SANGER | ||
| JVM-3 | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay, IC50 = 14.2627 μM. | SANGER | ||
| AN3-CA | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50 = 14.9578 μM. | SANGER | ||
| VM-CUB-1 | Growth inhibition assay | Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50 = 15.1364 μM. | SANGER | ||
| A253 | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50 = 15.2834 μM. | SANGER | ||
| RPMI-7951 | Growth inhibition assay | Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50 = 16.1981 μM. | SANGER | ||
| NCI-H1563 | Growth inhibition assay | Inhibition of human NCI-H1563 cell growth in a cell viability assay, IC50 = 16.8253 μM. | SANGER | ||
| LB831-BLC | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50 = 17.1929 μM. | SANGER | ||
| ES8 | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay, IC50 = 17.3157 μM. | SANGER | ||
| NCI-H292 | Growth inhibition assay | Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50 = 17.4749 μM. | SANGER | ||
| OAW-42 | Growth inhibition assay | Inhibition of human OAW-42 cell growth in a cell viability assay, IC50 = 17.8823 μM. | SANGER | ||
| RCC10RGB | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 17.9578 μM. | SANGER | ||
| PC-3 | Growth inhibition assay | Inhibition of human PC-3 cell growth in a cell viability assay, IC50 = 18.0043 μM. | SANGER | ||
| HCC38 | Growth inhibition assay | Inhibition of human HCC38 cell growth in a cell viability assay, IC50 = 18.1031 μM. | SANGER | ||
| DEL | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay, IC50 = 18.387 μM. | SANGER | ||
| ABC-1 | Growth inhibition assay | Inhibition of human ABC-1 cell growth in a cell viability assay, IC50 = 18.5627 μM. | SANGER | ||
| SW756 | Growth inhibition assay | Inhibition of human SW756 cell growth in a cell viability assay, IC50 = 19.1351 μM. | SANGER | ||
| TE-6 | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 19.2103 μM. | SANGER | ||
| H-EMC-SS | Growth inhibition assay | Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50 = 19.4359 μM. | SANGER | ||
| HCT-116 | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50 = 19.668 μM. | SANGER | ||
| CHP-212 | Growth inhibition assay | Inhibition of human CHP-212 cell growth in a cell viability assay, IC50 = 19.7478 μM. | SANGER | ||
| SK-LU-1 | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50 = 19.753 μM. | SANGER | ||
| HT-3 | Growth inhibition assay | Inhibition of human HT-3 cell growth in a cell viability assay, IC50 = 20.028 μM. | SANGER | ||
| KG-1 | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 20.206 μM. | SANGER | ||
| ES1 | Growth inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 21.0048 μM. | SANGER | ||
| Ramos-2G6-4C10 | Growth inhibition assay | Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 21.7756 μM. | SANGER | ||
| IA-LM | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay, IC50 = 21.9694 μM. | SANGER | ||
| BHT-101 | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 22.0629 μM. | SANGER | ||
| OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 22.47 μM. | SANGER | ||
| SW1573 | Growth inhibition assay | Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 22.7934 μM. | SANGER | ||
| CHL-1 | Growth inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 23.2833 μM. | SANGER | ||
| BFTC-905 | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 23.2892 μM. | SANGER | ||
| TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 23.5782 μM. | SANGER | ||
| NCI-H358 | Growth inhibition assay | Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50 = 23.6477 μM. | SANGER | ||
| OVCAR-5 | Growth inhibition assay | Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50 = 24.104 μM. | SANGER | ||
| CGTH-W-1 | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 25.0804 μM. | SANGER | ||
| SNU-423 | Growth inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50 = 25.366 μM. | SANGER | ||
| CP50-MEL-B | Growth inhibition assay | Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 25.7399 μM. | SANGER | ||
| NCI-H2087 | Growth inhibition assay | Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 25.8655 μM. | SANGER | ||
| RMG-I | Growth inhibition assay | Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 25.9219 μM. | SANGER | ||
| KP-N-YS | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 26.202 μM. | SANGER | ||
| OMC-1 | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay, IC50 = 26.508 μM. | SANGER | ||
| DMS-114 | Growth inhibition assay | Inhibition of human DMS-114 cell growth in a cell viability assay, IC50 = 27.3966 μM. | SANGER | ||
| SHP-77 | Growth inhibition assay | Inhibition of human SHP-77 cell growth in a cell viability assay, IC50 = 27.488 μM. | SANGER | ||
| MPP-89 | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 27.9438 μM. | SANGER | ||
| NCI-H1581 | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 28.4535 μM. | SANGER | ||
| D-283MED | Growth inhibition assay | Inhibition of human D-283MED cell growth in a cell viability assay, IC50 = 28.4674 μM. | SANGER | ||
| MOLT-4 | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 28.9072 μM. | SANGER | ||
| ES6 | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 29.6436 μM. | SANGER | ||
| NB6 | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50 = 29.8638 μM. | SANGER | ||
| SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 29.9407 μM. | SANGER | ||
| A388 | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50 = 29.9422 μM. | SANGER | ||
| OAW-28 | Growth inhibition assay | Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 30.2278 μM. | SANGER | ||
| SK-MES-1 | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 31.2208 μM. | SANGER | ||
| NCI-H441 | Growth inhibition assay | Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 31.9868 μM. | SANGER | ||
| HOP-92 | Growth inhibition assay | Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 32.2356 μM. | SANGER | ||
| NB14 | Growth inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50 = 32.7251 μM. | SANGER | ||
| MS-1 | Growth inhibition assay | Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 32.7604 μM. | SANGER | ||
| YKG-1 | Growth inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 32.8336 μM. | SANGER | ||
| SiHa | Growth inhibition assay | Inhibition of human SiHa cell growth in a cell viability assay, IC50 = 33.3829 μM. | SANGER | ||
| HAL-01 | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 34.2376 μM. | SANGER | ||
| Ca-Ski | Growth inhibition assay | Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50 = 34.7669 μM. | SANGER | ||
| NCI-H747 | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 34.9875 μM. | SANGER | ||
| KYSE-510 | Growth inhibition assay | Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50 = 35.6485 μM. | SANGER | ||
| A204 | Growth inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50 = 35.7209 μM. | SANGER | ||
| HSC-3 | Growth inhibition assay | Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 36.0086 μM. | SANGER | ||
| HuP-T3 | Growth inhibition assay | Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 36.4832 μM. | SANGER | ||
| RPMI-8226 | Growth inhibition assay | Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 36.6208 μM. | SANGER | ||
| QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 36.644 μM. | SANGER | ||
| HuH-7 | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 38.6184 μM. | SANGER | ||
| CAL-12T | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 38.9416 μM. | SANGER | ||
| GT3TKB | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 39.1921 μM. | SANGER | ||
| OC-314 | Growth inhibition assay | Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 39.7125 μM. | SANGER | ||
| NCI-H2228 | Growth inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 40.1403 μM. | SANGER | ||
| NCI-H727 | Growth inhibition assay | Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 40.2531 μM. | SANGER | ||
| NTERA-S-cl-D1 | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 40.4706 μM. | SANGER | ||
| MMAC-SF | Growth inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50 = 40.9235 μM. | SANGER | ||
| HTC-C3 | Growth inhibition assay | Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 41.4169 μM. | SANGER | ||
| SF295 | Growth inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 41.5379 μM. | SANGER | ||
| U-2-OS | Growth inhibition assay | Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 41.8567 μM. | SANGER | ||
| HPAF-II | Growth inhibition assay | Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 41.9382 μM. | SANGER | ||
| KYSE-450 | Growth inhibition assay | Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 42.4707 μM. | SANGER | ||
| DMS-273 | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 43.2836 μM. | SANGER | ||
| HT-1376 | Growth inhibition assay | Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 43.3156 μM. | SANGER | ||
| 786-0 | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 43.6261 μM. | SANGER | ||
| NCI-H810 | Growth inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50 = 44.0136 μM. | SANGER | ||
| 8305C | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 44.645 μM. | SANGER | ||
| DSH1 | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50 = 45.7042 μM. | SANGER | ||
| KYSE-520 | Growth inhibition assay | Inhibition of human KYSE-520 cell growth in a cell viability assay, IC50 = 46.5721 μM. | SANGER | ||
| TYK-nu | Growth inhibition assay | Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 46.7092 μM. | SANGER | ||
| EPLC-272H | Growth inhibition assay | Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 46.7283 μM. | SANGER | ||
| T-24 | Growth inhibition assay | Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 47.9292 μM. | SANGER | ||
| BHY | Growth inhibition assay | Inhibition of human BHY cell growth in a cell viability assay, IC50 = 47.999 μM. | SANGER | ||
| NCI-H82 | Growth inhibition assay | Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 48.217 μM. | SANGER | ||
| SF268 | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50 = 48.6189 μM. | SANGER | ||
| C-33-A | Growth inhibition assay | Inhibition of human C-33-A cell growth in a cell viability assay, IC50 = 48.7554 μM. | SANGER | ||
| MIA-PaCa-2 | Growth inhibition assay | Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 48.8388 μM. | SANGER | ||
| HCC1954 | Growth inhibition assay | Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 49.0871 μM. | SANGER | ||
| NCI-H1666 | Growth inhibition assay | Inhibition of human NCI-H1666 cell growth in a cell viability assay, IC50 = 49.3642 μM. | SANGER | ||
| GR-ST | Growth inhibition assay | Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 49.3695 μM. | SANGER | ||
| Ca9-22 | Growth inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 49.4013 μM. | SANGER | ||
| D-502MG | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 49.417 μM. | SANGER | ||
| SCC-4 | Growth inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 49.5602 μM. | SANGER | ||
| RKO | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50 = 49.8356 μM. | SANGER | ||
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生物活性
| 製品説明 | RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis. | ||||||||
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| Targets |
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| In Vitro | ||||
| In vitro |
RO-3306 inhibits CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D activity with Ki of 35 nM, 110 nM, 340 nM, and over 2000 nM, respectively. Treatment of HCT116, SW480, and HeLa cells with RO-3306 for 20 h leads to a complete block of the cell cycle in the G2/M phase. The proliferation of both HCT116 and SW480 is effectively blocked by RO-3306. RO-3306 appears to be more proapoptotic in cancer cells (HCT116 and SW480) than nontumorigenic cells (MCF 10A and MCF 12A).[1] RO-3306 effectively arrests oocyte maturation at a concentration of 10 μM.[2] |
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| Kinase Assay | CDK assay | |||
| The activity of CDK1 cyclin B1, CDK1 cyclin A, CDK2 cyclin E, and CDK4 cyclin D is measured by a homogeneous time-resolved fluorescence assay in a 96-well format. The assay buffer contained 25 mM Hepes, 6.25 mM MgCl2, 0.003% Tween 20, 0.3 mg/mL BSA, 1.5 mM DTT, and ATP as follows: 162 μM (CDK1), 90 mM (CDK2), or 135 μM (CDK4). CDK1 and CDK2 buffer contained 10 mM MgCl2. Test compounds are diluted in assay buffer to 3-fold their final concentration in 20 μL, and the reaction is started by the addition of a 40 μL assay buffer containing the pRB substrate (0.185μM). The plates are incubated at 37°C for 30 min with constant agitation, and the reaction is terminated by the addition of 15 μL of 1.6μM anti-phospho pRB antibody (Ser-780) in 25 mM Hepes, 24 mM EDTA, and 0.2 mg/mL BSA. After an additional 30 min of incubation with shaking, 15μL of 3nM Lance-Eu-W1024-labeledanti-rabbitIgG and 60 nM Alophycocyanin-conjugated anti-His-6 antibody in 25 mM Hepes, and 0.5 mg/mL BSA is added and incubated for 1 h. The plates are read in the Victor-V multi- label reader at excitation 340 nm and emission 615 nm and 665 nm. The IC50 values are calculated from the readings at 665 nm and normalized for Europium readings at 615 nm. Ki values are calculated according to the equation: Ki= IC50/(1 + S/Km ), where S is the ATP concentration in the assay and Km is the Michaelis-Menten constant for ATP. The inhibitory activity against the panel of kinases is determined by the IMAP assay technology. | ||||
| 細胞実験 | 細胞株 | MDA-MB-231 cell line | ||
| 濃度 | 20 μM | |||
| 反応時間 | 72 h | |||
| 実験の流れ | Log phases cells (25,000) are seeed in 96-well plates and incubated in a 37℃ incubator with CO2, After 24 h, different concentrations of RO-3306 are administered to determine the drug concentrations required to achieve a 50% growth inhibition (IC50). MTT (20 μL, 5mg/mL stock solution in saline) is added to each well and the cells are incubated for 4 h. Supernatants are removed and formazan crystals from viable cells are solubilized with 200 μL anhydrous DMSO. The absorbance is detected with a 550 model microplate reader at the 565 nm wavelength. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-Cdk1 / Cdk1 / Cleaved PARP / Cleaved caspase-3 / p-p38 / Bad / Apaf1-1 / p-H2Ax / Bim / Bad |
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27385216 | |
| Immunofluorescence | PARP1 / Plk1 |
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28069876 | |
| Growth inhibition assay | Cell viability |
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27385216 | |
| In Vivo | ||
| In Vivo |
RO-3306 is an ATP-competitive, and selective CDK1 inhibitor. |
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| 動物実験 | 動物モデル | Female BALB/c mice |
| 投与量 | 1.5 mg/kg | |
| 投与経路 | i.n. | |
化学情報
| 分子量 | 351.45 | 化学式 | C18H13N3OS2 |
| CAS No. | 872573-93-8 | SDF | Download Ro-3306 SDFをダウンロードする |
| Smiles | C1=CC2=C(C=CC(=C2)C=C3C(=O)NC(=NCC4=CC=CS4)S3)N=C1 | ||
| 保管 | |||
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In vitro |
DMSO : 70 mg/mL ( (199.17 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
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in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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