Samuraciclib hydrochloride (ICEC0942 hydrochloride)

Catalog No.S8722 Synonyms: CT7001 hydrochloride

For research use only.

Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 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 apoptosis.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) Chemical Structure

CAS No. 1805789-54-1

Selleck's Samuraciclib hydrochloride (ICEC0942 hydrochloride) has been cited by 1 Publication

Purity & Quality Control

Choose Selective CDK Inhibitors

Other CDK Products

Biological Activity

Description Samuraciclib hydrochloride (ICEC0942 hydrochloride, CT7001 hydrochloride) is a new, orally bioavailable CDK7 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 apoptosis.
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[1].

Assay
Methods Test Index PMID
Western blot p-Ser2 PolII / p-Ser5 PolII / p-Ser7 PolII / p-CDK7 / CDK7 / p-RB 29545334
In vivo

In xenografts of both breast and colorectal cancers, ICEC0942 has substantial anti-tumor effects. For pharmacokinetics, CD1 male mice are treated intravenously (IV), subcutaneously (SC) or by oral gavage (PO) with 10 mg/kg ICEC0942. In plasma, ICEC0942 levels decline in a bi-phasic manner, indicating rapid distribution into tissues. Following IV administration of ICEC0942 at 10 mg/kg in male CD1 mice Cl(plasma) is calculated at 78 ml.min/kg. Blood/plasma ratio (Bl/Pl) is 1.81. ICEC0942 has a half-life of 1.9 hrs, a moderate half-life in this species. Only a small proportion (13.5%) of ICEC0942 is metabolized after 2 and 4 hour following a single PO administration (100 mg/kg). Comparing exposure (AUCt) after single PO and IV administration at 10 mg/kg, oral bioavailability (F%) is calculated at 30%. Median Tmax for PO administration is 2 hours and is unaffected by increasing dose. Over this dose range, Cmax is linearly associated with dose, as is the total exposure over time (AUCt). In tumor-bearing mice, there is appreciable accumulation of ICEC0942 in tumors 6-hours post administration. ICEC0942 levels in tumors lag behind plasma levels[1].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: HCT116 cells
  • Concentrations: 0.1, 1, 10 μM
  • Incubation Time: 4, 8, 16, 24 h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: seven-week old female nu/nu-BALB/c athymic nude mice with tumour xenograft
  • Dosages: 100 mg/kg/day
  • Administration: PO

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 430.97
Formula

C22H31ClN6O

CAS No. 1805789-54-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCC4CCNCC4O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Samuraciclib hydrochloride (ICEC0942 hydrochloride) | Samuraciclib hydrochloride (ICEC0942 hydrochloride) supplier | purchase Samuraciclib hydrochloride (ICEC0942 hydrochloride) | Samuraciclib hydrochloride (ICEC0942 hydrochloride) cost | Samuraciclib hydrochloride (ICEC0942 hydrochloride) manufacturer | order Samuraciclib hydrochloride (ICEC0942 hydrochloride) | Samuraciclib hydrochloride (ICEC0942 hydrochloride) distributor