| Identification | Back Directory | [Name]
2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- | [CAS]
2479306-60-8 | [Synonyms]
CDK9-IN-19
2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- | [Molecular Formula]
C26H22F2N4O5 | [MOL File]
2479306-60-8.mol | [Molecular Weight]
508.47 |
| Hazard Information | Back Directory | [Uses]
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML)[1]. | [in vivo]
CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model[1].
Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice[1].
| PO (30 mg/kg) | IV (2 mg/kg) | | T1/2 (h) | NR | 0.23 | | Tmax (h) | 0.25 | - | | C0 (ng/mL) | - | 3060 | | Cmax (ng/mL) | 665 | - | | AUC0-t (ng/mL·h) | 1200 | 560 | | AUC0-∞ (ng/mL·h) | NR | 561 | | CL (L/h/kg) | - | 3.56 | | VdSS (L/kg) | - | 0.67 | | F (%) | 14.3 | - |
| Animal Model: | Female BALB/c nude mice (injected with MV4-11)[1] | | Dosage: | 10, 20 or 40 mg/kg | | Administration: | IV, for 32 days | | Result: | Significantly suppressed the tumour progression and tumour growth inhibition (TGI) values up to 100% from days 14-32 at 40 mg/kg. |
| [IC 50]
CDK9/cyclinT1: 2 nM (IC50) | [References]
[1] Xu J, et al. Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity. Eur J Med Chem. 2020 Aug 15;200:112424. DOI:10.1016/j.ejmech.2020.112424 |
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