2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- manufacturers
- CDK9-IN-19
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- $1980.00
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2026-07-27
- CAS:2479306-60-8
- Purity:
- Supply Ability: 10g
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| | 2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- Basic information |
| | 2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- Chemical Properties |
| Boiling point | 682.9±65.0 °C(Predicted) | | density | 1.425±0.06 g/cm3(Predicted) | | pka | 0.35±0.10(Predicted) |
| | 2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- Usage And Synthesis |
| 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 |
| | 2H-1-Benzopyran-2-one, 3-acetyl-7-[[5-fluoro-4-(4-fluoro-2-methoxyphenyl)-2-pyrimidinyl]amino]-4-(4-morpholinyl)- Preparation Products And Raw materials |
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