THAL-SNS-032
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- CAS番号.
- 2139287-33-3
- 化学名:
- 别名:
- 英語名:
- THAL-SNS-032
- 英語别名:
- SNS-THAL-032;THAL-SNS-032;THAL SNS 032,inhibit,PROTACs,CDK,THALSNS032,Cyclin dependent kinase,Inhibitor;N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide;1-Piperidineacetamide, 4-[[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]carbonyl]-N-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]-
- CBNumber:
- CB64668606
- 化学式:
- C40H52N8O10S2
- 分子量:
- 869.02
- MOL File:
- 2139287-33-3.mol
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THAL-SNS-032 物理性質
- 比重(密度) :
- 1.40±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- Store at -20°C, stored under nitrogen
- 溶解性:
- DMSO : 100 mg/mL (115.07 mM; Need ultrasonic)
- 酸解離定数(Pka):
- 7.86±0.70(Predicted)
- InChIKey:
- BXDZOYLPNAIDOC-UHFFFAOYSA-N
- SMILES:
- N1(CC(NCCOCCOCCOCCNC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)=O)CCC(C(NC2=NC=C(SCC3=NC=C(C(C)(C)C)O3)S2)=O)CC1
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
THAL-SNS-032 価格
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THAL-SNS-032 化学特性,用途語,生産方法
使用
THAL SNS 032 is a potent, selective and cereblon-dependent degrader of CDK9 (EC50 = 4 nM). Displays >15-fold selectivity for CDK9 over other CDKs (EC50 values are 62, 171 and 398 nM for CDK2, CDK1 and CDK7, respectively). Induces complete degradation of CDK9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.
生物活性
THAL-SNS-032, a small molecule formed by conjugating the multi-targeting kinase inhibitor SNS-032 to thalidomide, induced potent and selective degradation of CDK9 in a CRBN-dependent fashion. Treatment with THAL-SNS-032 resulted in selective degradation of CDK9 with limited effects on the protein level of other CDKs. Furthermore, THAL-SNS-032 had a prolonged pharmacodynamic effect compared with traditional kinase inhibitors. The antitumoral activity of THAL-SNS-032 in cell lines expressing ER or both ER and HER2, including luminal A cells, has been demonstrated[1-2].
THAL-SNS-032 上流と下流の製品情報
原材料
準備製品
THAL-SNS-032 生産企業
Global( 62)Suppliers
- 2139287-33-3
- THAL-SNS-032
- N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide
- 1-Piperidineacetamide, 4-[[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]carbonyl]-N-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]-
- SNS-THAL-032
- THAL SNS 032,inhibit,PROTACs,CDK,THALSNS032,Cyclin dependent kinase,Inhibitor