| Identification | Back Directory | [Name]
CDKI-73 | [CAS]
1421693-22-2 | [Synonyms]
CDKI-73
CS-2259
CDKI-73
(CDKI73)
Benzenesulfonamide, 3-[[5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]- | [Molecular Formula]
C15H15FN6O2S2 | [MDL Number]
MFCD28386217 | [MOL File]
1421693-22-2.mol | [Molecular Weight]
394.45 |
| Chemical Properties | Back Directory | [Boiling point ]
642.9±65.0 °C(Predicted) | [density ]
1.524±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:52.0(Max Conc. mg/mL);131.83(Max Conc. mM) | [form ]
Solid | [pka]
10.06±0.60(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
3-[[5-Fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]benzenesulfonamide is a potent CDK inhibitor. A highly efficacious CDK9 inhibitor against acute myeloid leukemia. | [in vivo]
Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities.[3].
| Animal Model: | MV4-11 tumor bearing mice[3]. | | Dosage: | 25 mg/kg. | | Administration: | Orally once everyday for 33 days. | | Result: | Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31. |
| Animal Model: | Balb/C mice aged 6-8 weeks[3]. | | Dosage: | 2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.) | | Administration: | IV and PO, single dose. | | Result: | The Cmax increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg.
CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oral
bioavailability (F) ranged from 54 to 85% across the three doses.
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| [IC 50]
CDK2: 3.27 nM (IC50); CDK9: 5.78 nM (IC50); CDK1: 8.17 nM (IC50); CDK4: 8.18 nM (IC50); CDK6: 37.68 nM (IC50); CDK7: 134.26 nM (IC50); CDK1: 4 nM (Ki); CDK2: 3 nM (Ki); CDK9: 4 nM (Ki); CDK7: 91 nM (Ki) |
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