- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
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- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
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TAE684 (NVP-TAE684)
TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
CAS No. 761439-42-3
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製品安全説明書
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TAE684 (NVP-TAE684)関連製品
シグナル伝達経路
ALK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| SCC-3 | Growth Inhibition Assay | IC50=0.0000603 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=0.000564 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=0.000927 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=0.00162 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=0.00277 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.02384 μM | SANGER | ||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=0.02952 μM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.04865 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.05565 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=0.10256 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.10294 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.10568 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.16096 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=0.16478 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=0.17443 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=0.17835 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.19343 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.19631 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.19692 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.19776 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=0.22669 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.23524 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.24524 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=0.2553 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.27855 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.29159 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.30218 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.31204 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=0.31787 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=0.32523 μM | SANGER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=0.33123 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.33291 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=0.33303 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.33396 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=0.36988 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=0.38867 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.39446 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.39561 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.40569 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.41292 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.41609 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=0.4288 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.43215 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=0.43826 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=0.47116 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=0.47375 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=0.48142 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.48328 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.49031 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.49109 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=0.4989 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=0.50112 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.51124 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.53349 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.54549 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=0.55023 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.55184 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.55624 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=0.55794 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=0.56724 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=0.57884 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.63526 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=0.6358 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=0.63725 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.65033 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=0.66168 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=0.66169 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=0.67462 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=0.69074 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=0.69389 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=0.71496 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.72664 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=0.74975 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=0.76695 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=0.77559 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.82375 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=0.83233 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=0.83912 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=0.84042 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.84263 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=0.85863 μM | SANGER | ||
| CHP-126 | Growth Inhibition Assay | IC50=0.85957 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.87589 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=0.89757 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.90739 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=0.95526 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=0.98824 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.9884 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.99535 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=1.00639 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=1.03076 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=1.05063 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=1.06274 μM | SANGER | ||
| NCI-H716 | Growth Inhibition Assay | IC50=1.07259 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=1.08819 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=1.09798 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=1.10022 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=1.11328 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=1.11568 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=1.13112 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.13338 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=1.14895 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.15283 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.15974 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=1.19567 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=1.22379 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=1.2389 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=1.25208 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=1.26348 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=1.29117 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=1.32689 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=1.3408 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.34489 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=1.34986 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=1.36143 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=1.36378 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=1.37293 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=1.38757 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=1.45853 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=1.46659 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=1.49922 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=1.51594 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=1.55811 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=1.5613 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=1.5696 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=1.57113 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=1.57392 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=1.58476 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=1.6085 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=1.6319 μM | SANGER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=1.64307 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.6866 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.69573 μM | SANGER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=1.70036 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=1.73842 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=1.76272 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.78309 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=1.78967 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=1.85096 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=1.851 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=1.86241 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=1.87143 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=1.98299 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=2.00555 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.01513 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=2.03351 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=2.06786 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=2.11559 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=2.12445 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=2.17683 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=2.1905 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=2.19141 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=2.20041 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=2.22269 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.33256 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=2.37493 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=2.39972 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=2.42341 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=2.43674 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.47467 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=2.61524 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=2.63641 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=2.65414 μM | SANGER | ||
| BOKU | Growth Inhibition Assay | IC50=2.72764 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=2.79912 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=2.81804 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=2.82012 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=2.9617 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=3.08862 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=3.13203 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=3.18943 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=3.2002 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=3.26859 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=3.28797 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=3.32849 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=3.33544 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=3.53883 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=3.62028 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=3.64088 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=3.66434 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=3.6871 μM | SANGER | ||
| ECC4 | Growth Inhibition Assay | IC50=3.7756 μM | SANGER | ||
| ARH-77 | Growth Inhibition Assay | IC50=4.11067 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=4.13068 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=4.2619 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=4.27419 μM | SANGER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=4.28443 μM | SANGER | ||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=4.30601 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=4.47336 μM | SANGER | ||
| DMS-153 | Growth Inhibition Assay | IC50=4.66475 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=4.68515 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=4.76248 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=4.86196 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=4.87227 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=4.94126 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=4.96439 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=4.97721 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=5.05323 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=5.1183 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=5.14268 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=5.17504 μM | SANGER | ||
| NCI-H1522 | Growth Inhibition Assay | IC50=5.26322 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=5.43633 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=5.47087 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=5.58034 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=5.58659 μM | SANGER | ||
| REH | Growth Inhibition Assay | IC50=6.25618 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=6.42791 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=6.60674 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=7.06492 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=7.22977 μM | SANGER | ||
| NCI-H322M | Growth Inhibition Assay | IC50=7.33335 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=7.54899 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=7.69215 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=8.01734 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=8.47066 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=8.55396 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=8.64006 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=8.89892 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=9.19157 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=9.21219 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=9.65396 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=9.7877 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=10.2347 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=10.3192 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=10.3972 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=10.8669 μM | SANGER | ||
| K052 | Growth Inhibition Assay | IC50=10.9322 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=10.9939 μM | SANGER | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis. | ||
|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro |
TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. [1] TAE684 markedly overcomes resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis.[2] Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM. [3] |
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|---|---|---|---|---|
| Kinase Assay | In vitro Enzyme Assays. | |||
| All in vitro enzyme assays are done at Upstate Biotechnology with the exception of InsR and IGF-1R. To determine the IC50 of TAE684 against InsR and IGF-1R a homogeneous time-resolved fluorescence assay is performed. ATP (10 mM) and 20 mg/ml biotinylated PolyEY (Glu, Tyr 4:1) are combined with 50 nL of serial dilutions of TAE684 (10-500 nM) and 4 ng of InsR enzyme in the presence of the kinase reaction buffer (20 mM Tris譎Cl, pH 7.5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA). Assays are incubated for 1 hour at ambient temperature. Reactions are terminated by adding 10 mL of the detection solution containing 50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/mL Eu3+ cryptate-labeled anti-phosphotyrosine antibody Mab PT66-K, and 5 mg/mL Streptavidin-XLent. The reaction is incubated for half an hour, and fluorescence signals are read on Analyst GT. | ||||
| 細胞実験 | 細胞株 | Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs. | ||
| 濃度 | 1 nM-10 μM | |||
| 反応時間 | 2–3 days | |||
| 実験の流れ | Cells are seeded in 384-well plates (2.5×104 cells per well) and incubated with serial dilutions of TAE684 or DMSO for 2–3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Growth inhibition assay | Cell viability |
|
18594010 | |
| Western blot | p-ROS1 / ROS1 p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP |
|
25351743 | |
| In Vivo | ||
| In Vivo |
After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. [1] TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors. [2] Furthermore, treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q. [3] |
|
|---|---|---|
| 動物実験 | 動物モデル | Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice. |
| 投与量 | 1, 3, and 10 mg/kg | |
| 投与経路 | Once daily by oral gavage for 3 weeks | |
化学情報
| 分子量 | 614.2 | 化学式 | C30H40ClN7O3S |
| CAS No. | 761439-42-3 | SDF | Download TAE684 (NVP-TAE684) SDFをダウンロードする |
| Smiles | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC | ||
| 保管 | |||
|
In vitro |
DMSO : 10 mg/mL ( (16.28 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 |
|
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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