2-Pyrimidinamine, N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]- manufacturers
- CDK4/6-IN-15
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- $2420.00
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2026-07-27
- CAS:2078047-99-9
- Purity:
- Supply Ability: 10g
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| | 2-Pyrimidinamine, N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]- Basic information |
| | 2-Pyrimidinamine, N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]- Chemical Properties |
| Boiling point | 641.3±65.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | pka | 9.16±0.20(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | 2-Pyrimidinamine, N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]- Usage And Synthesis |
| Uses | CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression[1]. | | in vivo | CDK4/6-IN-15 (compound 91) (2 mg/kg for i.v. or 10 mg/kg for p.o.; single dose) shows comparable oral absorption in healthy male adult BALB/c mice (20-25 g) as well as (5 mg/kg for i.v. or 200 mg/kg for p.o.; single dose) in male albino Wistar rats (250-350 g)[1].
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | CL (mL/min/kg) | Vss (L/kg) | AUC (μM·h) | Cmax (μM) | Tmax (h) | t1/2 (h) | F (%) | | rat | IV | 5 | 155 | 27.5 | 1.2 | 1.4 | / | 2.1 | / | | PO | 20 | / | / | 4.4 | 0.3 | 4.3 | 20.3 | 95 | | mouse | IV | 2 | 90 | 15.7 | 0.7 | 1.3 | / | 2.9 | / | | PO | 10 | / | / | 4.3 | 0.6 | 2.5 | 2.7 | 129 |
| | IC 50 | CDK4: 3 nM (IC50); CDK6: 0.279 μM (IC50); CDK2: 3.335 μM (IC50) | | References | [1] Tadesse S, et al. Discovery and pharmacological characterization of a novel series of highly selective inhibitors of cyclin-dependent kinases 4 and 6 as anticancer agents. Br J Pharmacol. 2018 Jun;175(12):2399-2413. DOI:10.1111/bph.13974 |
| | 2-Pyrimidinamine, N-[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]-5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]- Preparation Products And Raw materials |
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