CCT244747

CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.

Product Specifications

CAS Number

[1404095-34-6]

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

Target

Checkpoint Kinase (Chk)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CCT244747.html

Purity

99.46

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

N#CC1=NC=C(NC2=NC=C(C3=CN(C)N=C3)C(OC)=C2)N=C1O[C@H](C)CN(C)C

Molecular Formula

C20H24N8O2

Molecular Weight

408.46

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[1]Lainchbury M, et al. Discovery of 3-alkoxyamino-5- (pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. J Med Chem. 2012 Nov 26;55 (22) :10229-40.|[2]Walton MI, et al. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clin Cancer Res. 2012 Oct 15;18 (20) :5650-61.|[3]Patel R, et al. An orally bioavailable Chk1 inhibitor, CCT244747, sensitizes bladder and head and neck cancer cell lines to radiation. Radiother Oncol. 2017 Mar;122 (3) :470-475.