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Chemical Structure : CDDD11-8
Catalog No.: PC-21462Not For Human Use, Lab Use Only.
CDDD11-8 is a potent, selective, orally bioavailable CDK9 inhibitor with Ki of 8 nM, shows >50-fold selectivity over other CDKs, also inhibits FLT3-ITD with Ki of 13 nM.
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CDDD11-8 is a potent, selective, orally bioavailable CDK9 inhibitor with Ki of 8 nM, shows >50-fold selectivity over other CDKs, also inhibits FLT3-ITD with Ki of 13 nM.
CDDD11-8 also inhibits TRKC, FLT3, NUAK1, GLK, MINK, TNIK, and MST1 with Ki of 10 to 46 nM in a panel of 369 human kinases.
CDDD11-8 exhibits potent anti-proliferative effects leukemic cells that harbored the FLT3-ITD mutation and MLL fusions, such as MV4-11 (FLT3ITD/ITD/MLL-AF4) and MOLM-13 (FLT3ITD/WT/MLL-AF9), and those driven by TRK fusions (e.g., MO91) with GI50 values of < 0.1 uM.
CDDD11-8 (1 µM) decreases the level of total RNAP II and tubulin, suppresses the expressions of c-MYC, MCL-1, and XIAP in MV4-11 and MOLM-13 cells.
CDDD11-8 (75 and 125 mg/kg, PO, QD) demonstrates tumor growth inhibition efficacy against MV4-11 tumor xenografts.
CDDD11-8 also has efficacy in TNBC without apparent toxicity to normal tissues.
| M.Wt | 398.51 | |
| Formula | C24H26N6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Abel Tesfaye Anshabo, et al. Cancers (Basel). 2022 Feb 22;14(5):1113.
2. Mustafa EH, et al. Oncogene. 2023 Nov 24. doi: 10.1038/s41388-023-02892-3.
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