For research use only. Not for therapeutic Use.
CCT244747（Cat No.:I001550）is a selective inhibitor of the protein kinase ATR (ataxia telangiectasia and Rad3-related), which plays a crucial role in the cellular response to DNA damage and replication stress. By inhibiting ATR, CCT244747 disrupts the repair of DNA double-strand breaks, leading to increased sensitivity of cancer cells to DNA-damaging agents, such as chemotherapy and radiation. This compound has shown potential in preclinical studies, particularly for tumors with deficiencies in DNA repair pathways, making it a candidate for enhancing the efficacy of cancer treatments and improving therapeutic outcomes in various malignancies.
| Catalog Number | I001550 |
| CAS Number | 1404095-34-6 |
| 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 |
| Molecular Formula | C₂₀H₂₄N₈O₂ |
| Purity | ≥95% |
| Target | Checkpoint Kinase (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 | C[C@H](CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C(C(=C2)OC)C3=CN(N=C3)C |
| Reference | </br>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 Article</br>2: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 |
