[CAS NO. 1805789-54-1] Samuraciclib hydrochloride (ICEC0942 hydrochloride)

Name: Samuraciclib hydrochloride (ICEC0942 hydrochloride)
Brand: Arctom Scientific
SKU: SLK-S8722

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PRODUCTS SPECIFICATIONS [1805789-54-1]

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Catalog

SLK-S8722

Brand

Selleck

CAS

1805789-54-1

DESCRIPTION [1805789-54-1]

Overview

MDL	-
Molecular Weight	430.97
Molecular Formula	C22H31ClN6O
SMILES	O[C@H]1CNCC[C@@H]1CNC2=NC3=C(C(C)C)C=NN3C(NCC4=CC=CC=C4)=C2.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3203 mL	11.6017 mL	23.2035 mL
5 mM	0.4641 mL	2.3203 mL	4.6407 mL
10 mM	0.2320 mL	1.1602 mL	2.3203 mL
50 mM	0.0464 mL	0.2320 mL	0.4641 mL

Description

Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and .

Targets

CDK7 ^[1] (Cell-free assay)	CDK2 ^[1] (Cell-free assay)	CDK9 ^[1] (Cell-free assay)	CDK1 ^[1] (Cell-free assay)
40 nM	620 nM	1.2 μM	1.8 μM

In vitro

A wide range of cancer types are sensitive to CDK7 inhibition by ICEC0942 with GI50 values ranging between 0.2-0.3 µM. ICEC0942 inhibits PolII, CDK1, CDK2 and RB (retinoblastoma) phosphorylation in the MCF7 breast cancer cell line in a time and dose-sependent manner. ICEC0942 inhibits phosphorylation of CDK7 substrates and promotes cell cycle arrest and apoptosis.

References

[1] Patel H, et al. Mol Cancer Ther. 2018, 17(6):1156-1166.