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Chemical Structure : CG13250
Catalog No.: PC-20160Not For Human Use, Lab Use Only.
CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).
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CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).
CG13250 inhibits the cell growth of MV4;11 cells with GI50 of 595 nM.
CG13250 is very selective for the Group II bromodomain-containing proteins (BCPs), which are the BET proteins, inhibiting all of them -many completely- at 10 uM, also significantly inhibits BRD9, BRPF1, CREBBP and EP300.
CG13250 displays high selectivity against 408 non-mutant kinases using DiscoverX's KINOMEscanTM platform.
CG13250 inhibits the binding of BRD4 to c-MYC promoter regions suppressing the transcription of the c-MYC gene.
CG13250 (25 mg/kg, PO, qD) prolongs the survival of in a subcutaneous murine model of a Kasumi-1 xenograft tumor for leukemia, with no body weight loss.
| M.Wt | 345.40 | |
| Formula | C21H19N3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jay Chauhan, et al. Bioorg Med Chem Lett. 2023 Mar 9;129220.
2. Imayoshi N, et al. Biochem Biophys Res Commun. 2017 Mar 4;484(2):262-268.
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