CCT244747

• CAT Number: I001550
• CAS Number: 1404095-34-6
• Molecular Formula: C₂₀H₂₄N₈O₂
• Molecular Weight: 408.46
• Purity: ≥95%
• Synonyms: (R)-3-((1-(dimethylamino)propan-2-yl)oxy)-5-((4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)pyrazine-2-carbonitrile
• Target: Chk
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: 3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-methoxy-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]pyrazine-2-carbonitrile
• InChI: InChI=1S/C20H24N8O2/c1-13(11-27(2)3)30-20-16(7-21)22-10-19(26-20)25-18-6-17(29-5)15(9-23-18)14-8-24-28(4)12-14/h6,8-10,12-13H,11H2,1-5H3,(H,23,25,26)/t13-/m1/s1
• InChIKey: IENLGMOXAQMNEH-CYBMUJFWSA-N
• SMILES: CC(CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C(C(=C2)OC)C3=CN(N=C3)C

CCT244747 (Cat.No:I001550) is a potent and selective inhibitor of checkpoint kinase 1 (Chk1), with an IC50 of 29 nM. It shows little activity against other kinases such as Chk2 and CDK2. In vitro studies have shown that CCT244747 can enhance the cytotoxicity of DNA-damaging agents in cancer cells. In vivo studies have also demonstrated its ability to sensitize tumor cells to radiation and chemotherapy. CCT244747 is being investigated as a potential anti-cancer therapeutic agent.

Reference

1:An orally bioavailable Chk1 inhibitor, CCT244747, sensitizes bladder and head and neck cancer cell lines to radiation. Patel R, Barker HE, Kyula J, McLaughlin M, Dillon MT, Schick U, Hafsi H, Thompson A, Khoo V, Harrington K, Zaidi S.Radiother Oncol. 2017 Mar;122(3):470-475. doi: 10.1016/j.radonc.2016.12.026. Epub 2017 Jan 25. PMID: 28131548 Free Article2:CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD.Clin Cancer Res. 2012 Oct 15;18(20):5650-61. doi: 10.1158/1078-0432.CCR-12-1322. Epub 2012 Aug 28. PMID: 22929806 Free PMC Article