ChemicalBook > CAS DataBase List > CDKI-73
CDKI-73
- Product Name
- CDKI-73
- CAS No.
- 1421693-22-2
- Chemical Name
- CDKI-73
- Synonyms
- CS-2259;CDKI-73;asnuciclib;CDKI-73 ,S7773;CDKI-73 (CDKI73);Asnuciclib (CDKI-73);CDKI-73, 10 mM in DMSO;3-((5-Fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-yl)amino)benzenesulfonamide;3-[[5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]-benzenesulfonamide;Benzenesulfonamide, 3-[[5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]-
- CBNumber
- CB53034461
- Molecular Formula
- C15H15FN6O2S2
- Formula Weight
- 394.45
- MOL File
- 1421693-22-2.mol
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CDKI-73 Property
- 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
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N-Bromosuccinimide Price
ChemScene
- Product number
- CS-3953
- Product name
- CDKI-73
- Purity
- 99.58%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-3953
- Product name
- CDKI-73
- Purity
- 99.58%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
Biorbyt Ltd
- Product number
- orb611582
- Product name
- CDKI-73
- Packaging
- 100mg
- Price
- $1060.8
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-3953
- Product name
- CDKI-73
- Purity
- 99.58%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
Biorbyt Ltd
- Product number
- orb611582
- Product name
- CDKI-73
- Packaging
- 250mg
- Price
- $2097.8
- Updated
- 2021/12/16
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CDKI-73 Chemical Properties,Usage,Production
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. |
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)
CDKI-73 Preparation Products And Raw materials
Raw materials
Preparation Products
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