Carfilzomib (PR-171)

製品コード：S2853 純度：99.75%

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.

CAS No. 868540-17-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 59500	国内在庫あり
5mg	JPY 25500	国内在庫あり
50mg	JPY 85500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（223）

製品安全説明書

現在のバッチを見る：純度： 99.75%

99.75

Carfilzomib (PR-171)関連製品

関連ターゲット	20S proteasome	もっと見る
関連製品	MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib ONX-0914 (PR-957) Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	もっと見る

シグナル伝達経路

Proteasomeシグナル伝達経路

Proteasome阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
UMSCC-1	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
1483	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
UMSCC-22B	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
UMSCC-22A	Apoptosis Asssay	200 nM	24 h	induce the cell apoptosis co-treatment with ONX 0912	22929803
Jurkat	Apoptosis Asssay	8 nM	24/48 h	induces apoptosis, caspase activation, and PARP cleavage co-treatment with vorinostat	24801128
Jurkat	Growth Inhibition Assay	1-11nM	48 h	inhibits the cell proliferation co-treatment with vorinostat	24801128
U2932	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
SUDHL14	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
SUDHL16	Apoptosis Asssay	2.5–3.5 nM	48 h	enhances the cell death co-treatment with ACY1215	25239935
NCI-H929	Growth Inhibition Assay	0-100 nM	48 h	IC50 = 14 nM	25312543
MM.1S	Growth Inhibition Assay	0-100 nM	48 h	IC50 = 10 nM	25312543
SUDHL16	Apoptosis Asssay	2.0-4.0 nM	48 h	induces cell death co-treatment with obatoclax	22411899
SUDHL16	Function Assay	2.5 nM	24 h	activates JNK, inactivates AKT, up-regulates Noxa, and induces γH2A.X co-treatment with obatoclax	22411899
Granta	Growth Inhibition Assay	0-4 nM	48 h	induce cell death co-treatment with HADCIs	21750224
SUDHL16	Growth Inhibition Assay	1-4 nM	36 h	induce cell death co-treatment with HADCIs	20233973
MCF7	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
MDA-MB-468	Function assay	35 nM	4 hrs	Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis	27994734
MOLT4	Function assay		1 hr	Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay, IC50 = 0.0051 μM.	19348473
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.018 μM.	19348473
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.413 μM.	19348473
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay, IC50 = 0.01319 μM.	24767818
NCI-H929	Cytotoxicity assay		72 hrs	Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay, IC50 = 0.02132 μM.	24767818
CCRF-CEM	Antiproliferative assay		72 hrs	Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0061 μM.	26231162
RPMI8266	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8266 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0139 μM.	26231162
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0193 μM.	26231162
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM.	26231162
TOV21G	Antiproliferative assay		72 hrs	Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM.	26231162
RKO	Antiproliferative assay		72 hrs	Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0271 μM.	26231162
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM.	27765408
RPMI8226	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM.	27765408
LCL	Cytotoxicity assay		48 hrs	Cytotoxicity against human LCL cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.03 μM.	27994734
RD-ES	Cytotoxicity assay		48 hrs	Cytotoxicity against human RD-ES cells harboring p53 mutant assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.043 μM.	27994734
U266	Cytotoxicity assay		48 hrs	Cytotoxicity against human U266 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.06 μM.	27994734
WE68	Cytotoxicity assay		48 hrs	Cytotoxicity against human WE68 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.08 μM.	27994734
IMR90	Cytotoxicity assay		48 hrs	Cytotoxicity against human IMR90 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.13 μM.	27994734
MCF10A	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF10A cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM.	27994734
SKOV3	Cytotoxicity assay		48 hrs	Cytotoxicity against p53 deficient human SKOV3 cells assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM.	27994734
MDA-MB-468	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-468 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.33 μM.	27994734
HNDF	Cytotoxicity assay		48 hrs	Cytotoxicity against HNDF cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.35 μM.	27994734
KGN	Cytotoxicity assay		48 hrs	Cytotoxicity against human KGN cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.45 μM.	27994734
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 4.5 μM.	27994734
MM1S	Cytotoxicity assay		72 hrs	Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM.	28027531
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM.	28027531
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.0041 μM.	30165344
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.0044 μM.	30165344
RPMI8226	Cytotoxicity assay		48 hrs	Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay, IC50 = 0.0067 μM.	30165344
UMSCC-22A	Growth Inhibition Assay			IC50=38.7 ± 1.0 nM	22929803
R-Cal33	Growth Inhibition Assay			IC50=1112 nM	24915039
P-Cal33	Growth Inhibition Assay			IC50=17.3 nM	24915039
R-UMSCC-1	Growth Inhibition Assay			IC50=2294 nM	24915039
P-UMSCC-1	Growth Inhibition Assay			IC50=11.2 nM	24915039
UMSCC-22B	Growth Inhibition Assay			IC50=30.7 ± 9.3 nM	22929803
1483	Growth Inhibition Assay			IC50=50.5 ± 11.9 nM	22929803
UMSCC-1	Growth Inhibition Assay			IC50=34.6 ± 2.6 nM	22929803
Cal33	Growth Inhibition Assay			IC50=49.3 ± 8.9 nM	22929803
PCI-15A	Growth Inhibition Assay			IC50=70.4 ± 22.6 nM	22929803
PCI-15B	Growth Inhibition Assay			IC50=39.5 ± 11.0 nM	22929803
OSC-19	Growth Inhibition Assay			IC50=18.3 ± 4.2 nM	22929803
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
ANBL-6	Function assay			Inhibition of 20S proteasome activity in human ANBL-6 cells, IC50 = 0.01 μM.	29652143
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生物活性

製品説明

Targets

Proteasome ^[1]
(ANBL-6 cells)

5 nM

In Vitro
In vitro	Carfilzomib inhibits proliferation in a variety of cell lines and patient-derived neoplastic cells, including multiple myeloma, and induced intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). Carfilzomib reveals enhanced anti-MM activity, overcome resistance to other agents, and acts synergistically with (Dex). Carfilzomib shoes preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM. Short exposure to low-dose Carfilzomib leads to preferential binding specificity for the β5 constitutive 20S proteasome and the β5i immunoproteasome subunits. Measurement of caspase activity in ANBL-6 cells pulsed with Carfilzomib reveals substantial increases in caspase-8, caspase-9, and caspase-3 activity after 8 hours, giving a 3.2-, 3.9- and 6.9-fold increase, respectively, over control cells after 8 hours. In carfilzomib pulse-treated cells, the mitochondrial membrane integrity is decreased to 41% (Q1 + Q2), compared with 75% in vehicle-treated control cells. ^[1] In another study, Carfilzomib has also shown preclinical effectiveness against hematological and solid malignancies. ^[2] Carfilzomib directly inhibits osteoclasts formation and bone resorption. ^[3]
Kinase Assay	Enzyme-linked immunosorbent assay for subunit profiling of carfilzomib
Kinase Assay	ANBL-6 cells (2 × 10⁶/well) are plated in 96-well plates and treated with Carfilzomib doses from 0.001 to 10 μM for 1 hour. Cells are then lysed (20 mM Tris-HCl, 0.5 mM EDTA), and cleared lysates are transferred to polymerase chain reaction (PCR) plates. A standard curve is generated using untreated ANBL-6 cell lysates starting at a concentration of 6 μg protein/μL. The active site probe [biotin-(CH2)4-Leu-Leu-Leu-epoxyketone; 20 μM] is added and incubated at room temperature for 1 hour. Cell lysates are then denatured by adding 1% sodium dodecyl sulfate (SDS) and heating to 100°C, followed by mixing with 20 μL per well streptavidin-sepharose high-performance beads in a 96-well multiscreen DV plate and incubated for 1 hour. These beads are then washed with enzyme-linked immunosorbent assay (ELISA) buffer (PBS, 1% bovine serum albumin, and 0.1% Tween-20), and incubated overnight at 4°C on a plate shaker with antibodies to proteasome subunits. Antibodies used included mouse monoclonal anti-β1, anti-β2, anti-β1i, and anti-β5i, goat polyclonal anti-β2i, and rabbit polyclonal anti-β5 (affinity-purified antiserum against KLH-CWIRVSSDNVADLHDKYS peptide). The beads are washed and incubated for 2 hours with horseradish peroxidase-conjugated secondary goat antirabbit, goat antimouse or rabbit antigoat antibodies. After washing, the beads are developed using the supersignal ELISA picochemiluminescence substrate. Luminescent detection is performed. Raw luminescence is converted to μg/mL by comparison with the standard curve and expressed as the % inhibition relative to vehicle control. Curve fits are generated using the following nonsigmoidal dose-response equation: Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope)), where X is the logarithm of concentration, Y is the % inhibition, and EC50 is the dose showing 50% effect.
細胞実験	細胞株	WST-1, ANBL-6 cells
	濃度	100 nM
	反応時間	1 hour
	実験の流れ	WST-1 is used to determine the effects of proteasome inhibitor Carfilzomib on cell proliferation. The inhibition of proliferation is calculated in relation to parallel control cells that receives vehicle alone. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR = IC50(resistant cells)/IC50(sensitive cells). ANBL-6 cells pulsed with 100 nM carfilzomib are washed and suspended in PBS containing 5 μg/mL of JC-1, which exhibits potential-dependent accumulation in mitochondria. Analysis of the mitochondrial membrane potential-dependent color shift from 525 to 590 nm is carried out on a FacScan, and the data are analyzed with CellQuest software.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K caspase-9 / caspase-8 c-PARP / PARP / caspase-3 Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak Atg5 / Atg12 / Beclin-1 / LC3-II Noxa / Bik / Puma / Mcl-1 EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53 BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut HLA class I		24590311
	Growth inhibition assay	Cell viability		27655642

In Vivo
In Vivo	Carfilzomib moderately reduces tumor growth in an in vivo xenograft model. Carfilzomib effectively decreases multiple myeloma cell viability following continual or transient treatment mimicking. Carfilzomib increases trabecular bone volume, decreases bone resorption and enhances bone formation in non-tumor bearing mice. ^[3]
動物実験	動物モデル	Beige-nude-XID mice
	投与量	2.0 mg/kg
	投与経路	i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05552976	Recruiting	Relapsed or Refractory Multiple Myeloma	Bristol-Myers Squibb	January 10 2023	Phase 3
NCT05675449	Recruiting	Multiple Myeloma	Pfizer	December 14 2022	Phase 1
NCT05041933	Unknown status	Hematological Diseases	University Hospital Limoges	September 15 2021	--

参考
[1] Kuhn DJ, et al. Blood. 2007, 110(9), 3281-3290. [2] Kuhn DJ, et al. Curr Cancer Drug Targets. 2011, 11(3), 285-295. [3] Hurchla MA, et al. Leukemia. 2012. [4] Dasmahapatra G, et al. Mol Cancer Ther. 2011, 10(9), 1686-1697. + 展開

参考

[4] Dasmahapatra G, et al. Mol Cancer Ther. 2011, 10(9), 1686-1697.

+ 展開

化学情報

分子量	719.91	化学式	C₄₀H₅₇N₅O₇
CAS No.	868540-17-4	SDF	Download Carfilzomib (PR-171) SDFをダウンロードする
Smiles	CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (138.9 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。)

Ethanol : 50 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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よくある質問（FAQ）

質問1:
How should I prepare solution of Carfilzomib for ongoing in vivo study?

回答
This compound can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/ castor oil at 10 mg/ml as a clear solution.

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