| Identification | Back Directory | [Name]
1,4-Cyclohexanediamine, N1-[5-methyl-4-(6-phenylimidazo[1,2-a]pyridin-3-yl)-2-pyrimidinyl]-, trans- | [CAS]
2241659-94-7 | [Synonyms]
CDDD11-8 1,4-Cyclohexanediamine, N1-[5-methyl-4-(6-phenylimidazo[1,2-a]pyridin-3-yl)-2-pyrimidinyl]-, trans- | [Molecular Formula]
C24H26N6 | [MOL File]
2241659-94-7.mol | [Molecular Weight]
398.5 |
| Hazard Information | Back Directory | [Uses]
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation[1][2]. | [in vivo]
CDDD11-8 (0-125 mg/kg, PO, daily) induces tumor regression[1]. | Animal Model: | MV4-11 tumor-bearing mice[1] | | Dosage: | 75 or 125 mg/kg | | Administration: | PO, daily for 5 or 28 days | | Result: | Induced tumor regression. Potently inhibited the phosphorylation of RNAPII at Ser2 and Ser5, confirming the inhibition of CDK9 in vivo. Reduced phosphorylation of FLT3 at Tyr591 and STAT5 at Tyr 694. |
| [IC 50]
CDK9: 8 nM (Ki) | [References]
[1] Anshabo AT, et al. An Orally Bioavailable and Highly Efficacious Inhibitor of CDK9/FLT3 for the Treatment of Acute Myeloid Leukemia. Cancers (Basel). 2022 Feb 22;14(5):1113. DOI:10.3390/cancers14051113 [2] Mustafa EH, et al. Selective inhibition of CDK9 in triple negative breast cancer. Oncogene. 2023 Nov 24. DOI:10.1038/s41388-023-02892-3 |
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