THAL-SNS-032
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- CAS-Nr.
- 2139287-33-3
- Englisch Name:
- THAL-SNS-032
- Synonyma:
- 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
- Summenformel:
- C40H52N8O10S2
- Molgewicht:
- 869.02
- MOL-Datei:
- 2139287-33-3.mol
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THAL-SNS-032 Eigenschaften
- Dichte
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C, stored under nitrogen
- Löslichkeit
- DMSO : 100 mg/mL (115.07 mM; Need ultrasonic)
- pka
- 7.86±0.70(Predicted)
- Aggregatzustand
- Solid
- Farbe
- Light yellow to yellow
- 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
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
THAL-SNS-032 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
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.
Biologische Aktivität
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
THAL-SNS-032 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 64)Lieferanten
- 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
- 2139287-33-3
- C40H52N8O10S2
