| Name | Samuraciclib hydrochloride |
| 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. |
| 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. |
| 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.
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| Keywords | Samuraciclib Hydrochloride | Samuraciclib hydrochloride | Samuraciclib | PolII | phosphorylates | non-covalent | Inhibitor | inhibit | ICEC-0942 Hydrochloride | ICEC0942 Hydrochloride | ICEC-0942 | ICEC0942 | ICEC 0942 Hydrochloride | ICEC 0942 | deregulation | Cyclin dependent kinase | cycle | CT-7001 Hydrochloride | CT7001 Hydrochloride | CT-7001 | CT7001 | CT 7001 Hydrochloride | CT 7001 | CDK7 | CDK | ATP-competitive | Asp155 | arrest | Apoptosis | anti-tumor |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Dextran sulfate sodium salt (MW 4500-5500) | Sodium 4-phenylbutyrate | L-Ascorbic acid | Metronidazole | Sorafenib | Tributyrin | Salicylic acid | Oleic acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
