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Samuraciclib hydrochloride
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Purity:99.57%
Samuraciclib hydrochloride
Catalog No. T10898Cas No. 1805789-54-1
Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $116 | In Stock | |
| 5 mg | $247 | In Stock | |
| 10 mg | $396 | In Stock | |
| 25 mg | $662 | In Stock | |
| 50 mg | $942 | In Stock | |
| 100 mg | $1,280 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $273 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects. |
| Targets&IC50 | CDK1-CyclinA:1.8 μM, CDK2-CyclinA:578 nM, CDK7-CyclinH:41 nM, CDK9-CyclinT1:1.2 μM, CDK6-CyclinD1:34 μM, CDK5-p35 NCK:9.4 μM, CDK4-CyclinD1:49 μM |
| In vitro | Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can promote apoptosis. Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment can induce cell cycle arrest. Samuraciclib (ICEC0942; 0-10 μM; 0-24 hours; HCT116 cells) treatment inhibited the phosphorylation of PolII CTD in HCT116 colon cancer cells in a dose- and time-dependent manner. ICEC0942 also inhibits the phosphorylation of CDK1, CDK2 and retinoblastoma. Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 μM, 0.32 μM, 0.33 μM, 0.21 μM, 0.22 μM It is 0.67 μM and 1.25 μM. |
| In vivo | Samuraciclib (ICEC0942; 100 mg / kg; oral tube; daily; 14 consecutive days; female nu / nu-BALB / c athymic nude mice) treatment inhibited tumor growth by 60% on day 14 with a significant reduction in PolII Ser2 and Ser5 phosphorylation in PBMC and tumors. The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment showed complete stagnation of estrogen receptor (ER) positive tumor xenografts. |
| Alias | ICEC0942 hydrochloride, CT7001 hydrochloride |
| Molecular Weight | 430.97 |
| Formula | C22H31ClN6O |
| Cas No. | 1805789-54-1 |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 55 mg/mL (127.62 mM), Sonication is recommended. DMSO: 25 mg/mL (58.01 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O
H2O
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Keywords
CDKSamuraciclib hydrochlorideCT 7001ATP-competitiveSamuraciclibinhibitApoptosisderegulationInhibitorCT7001non-covalentphosphorylatesCT-7001 HydrochlorideICEC-0942anti-tumorCT 7001 HydrochlorideSamuraciclib HydrochlorideCT7001 HydrochlorideCT-7001ICEC0942 HydrochlorideICEC 0942 HydrochlorideAsp155ICEC-0942 HydrochloridecycleCDK7ICEC 0942arrestICEC0942PolIICyclin dependent kinase
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