ICEC0942 (CT7001)

Catalog No.S8722

ICEC0942 (CT7001) Chemical Structure

Molecular Weight(MW): 430.97

ICEC0942 (CT7001) 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.

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Description ICEC0942 (CT7001) 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.
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; 

PubMed: 29545334     


HCT116 cells were treated with ICEC0942 at concentrations shown. Cell lysates were prepared at the indicated time points following ICEC0942 addition.

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

Cell Research:

[2]

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

    --


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: seven-week old female nu/nu-BALB/c athymic nude mice with tumour xenograft
  • Formulation: 10% DMSO/PBS
  • Dosages: 100 mg/kg/day
  • Administration: PO
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.54 mM)
Water 86 mg/mL (199.54 mM)
Ethanol 15 mg/mL (34.8 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 430.97
Formula

C22H31ClN6O

CAS No. 1805789-54-1
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID