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Samuraciclib hydrochloride

Catalog No. T10898 CAS 1805789-54-1

Synonyms: ICEC0942 hydrochloride, CT7001 hydrochloride

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.

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Samuraciclib hydrochloride Chemical Structure

Samuraciclib hydrochloride, CAS 1805789-54-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 117.00
2 mg	In stock	$ 165.00
5 mg	In stock	$ 249.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 662.00
50 mg	In stock	$ 942.00
100 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 273.00

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Purity: 99.57%

Purity: 98.99%

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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	CDK6-CyclinD1:34 μM, CDK4-CyclinD1:49 μM, CDK9-CyclinT1:1.2 μM, CDK7-CyclinH:41 nM, CDK2-CyclinA:578 nM, CDK5-p35 NCK:9.4 μM, CDK1-CyclinA:1.8 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.

Synonyms	ICEC0942 hydrochloride, CT7001 hydrochloride
Molecular Weight	430.97
Formula	C22H31ClN6O
CAS No.	1805789-54-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 55 mg/mL (127.62 mM), Sonication is recommended.

DMSO: 25 mg/mL (58.01 mM), Sonication is recommended.

References and Literature

1. Patel H, et al. ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. Mol Cancer Ther. 2018 Jun;17(6):1156-1166. 2. Hazel P, et al. Inhibitor Selectivity for Cyclin-Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study. ChemMedChem. 2017 Mar 7;12(5):372-380.

Citations

1. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Orally Active Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Compound Library Clinical Compound Library

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Keywords

Samuraciclib hydrochloride 1805789-54-1 Apoptosis Cell Cycle/Checkpoint CDK CT 7001 ICEC0942 hydrochloride CT7001 hydrochloride ATP-competitive Samuraciclib inhibit deregulation Inhibitor CT7001 non-covalent phosphorylates CT-7001 Hydrochloride ICEC-0942 anti-tumor CT 7001 Hydrochloride Samuraciclib Hydrochloride CT7001 Hydrochloride CT-7001 ICEC0942 Hydrochloride ICEC 0942 Hydrochloride Asp155 ICEC-0942 Hydrochloride cycle CDK7 ICEC 0942 arrest ICEC0942 PolII Cyclin dependent kinase inhibitor

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