CDKI-73
- CAS No.
- 1421693-22-2
- Chemical Name:
- CDKI-73
- Synonyms
- CS-2259;CDKI-73;asnuciclib;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]-;toxicity,Inhibitor,low,AML,Acute,LS 007,myeloid,LS007,leukemia,CLL,Apoptosis,LS-007,endosome,Cyclin dependent kinase,CDKI73,CDKI-73,CDKI 73,inhibit,CDK
- CBNumber:
- CB53034461
- Molecular Formula:
- C15H15FN6O2S2
- Molecular Weight:
- 394.45
- MDL Number:
- MFCD28386217
- MOL File:
- 1421693-22-2.mol
- MSDS File:
- SDS
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 |
FDA UNII | 235XBY3N9F |
CDKI-73 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-3953 | CDKI-73 99.58% | 1421693-22-2 | 5mg | $420 | 2021-12-16 | Buy |
ChemScene | CS-3953 | CDKI-73 99.58% | 1421693-22-2 | 10mg | $600 | 2021-12-16 | Buy |
Biorbyt Ltd | orb611582 | CDKI-73 | 1421693-22-2 | 100mg | $1060.8 | 2021-12-16 | Buy |
ChemScene | CS-3953 | CDKI-73 99.58% | 1421693-22-2 | 50mg | $1800 | 2021-12-16 | Buy |
Biorbyt Ltd | orb611582 | CDKI-73 | 1421693-22-2 | 250mg | $2097.8 | 2021-12-16 | Buy |
CDKI-73 Chemical Properties,Uses,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
CDKI-73 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32202 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38636 | 58 | |
Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 12952 | 65 |