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CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) [1]. | [in vivo]
CDK/HDAC-IN-3 (compound 33a) (i.v., p.o.; 5, 25 mg/kg) has relatively adequate oral bioavailability[1].
| Animal Model: | Sprague-Dawley male rats (220-350 g)[1] | | Dosage: | 5 mg/kg and 25 mg/kg | | Administration: | IV and PO | | Result: | | PK parameters | i.v (5 mg/Kg) | p.o (25 mg/Kg) | | Cmax(ng/L) | 3644.00 | 1426.00 | | T1/2(h) | 0.11 | 1.37 | | TMax(h) | NA | 0.75 | | Clearance (mL/h/kg) | 5307.00 | 1726.00 | | MRT (h) | 0.39 | 1.27 | | AUC (ng.h/mL) | 836.00 | 2368.00 | | F% | NA | 56.70% |
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| [References]
[1] Liu Y, et al. Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells. Eur J Med Chem. 2023;249:115140. DOI:10.1016/j.ejmech.2023.115140 |
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