ARV-771
Cat. No.:YN430002
产品名称: | ARV-771 |
CAS No.: | 1949837-12-0 |
Chemical Name: | (2S,4R)-1-((S)-2-(tert-butyl)-15-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carbox |
Synonyms: | ARV 771; ARV771 |
分子量: | 986.64 |
分子式: | C₄₉H₆₀ClN₉O₇S₂ |
SMILES: | CC(C(C(C1=CC=C(Cl)C=C1)=N[C@@H](CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N(C[C@H](O)C2)[C@@H]2C(N[C@H](C3=CC=C(C(SC=N4)=C4C)C=C3)C)=O)=O)=O)=O)C5=NN=C(C)N65)=C6S7)=C7C |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | ARV-771 是一种 PROTAC 类的有效BET降解剂。对BRD2(1),BRD2(2),BRD3(1),BRD3(2),BRD4(1)和BRD4(2)的Kd值分别为 34 nM,4.7 nM,8.3 nM,7.6 nM,9.6 nM 和 7.6 nM。 |
IC50和靶点: | [{name:"BRD2(1):34 nM (Kd)"},{name: "BRD2(2):4.7 nM (Kd)"},{name: "BRD3(1):8.3 nM (Kd)"},{name: "BRD3(2):7.6 nM (Kd)"},{name: "BRD4(1):9.6 nM (Kd)"},{name: "BRD4(2):7.6 nM (Kd)"}] |
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Clinical Trial: | |
Solvent & Solubility: |
Raina, K., Lu, J., Qian, Y., et al.PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancerProc. Natl. Acad. Sci. USA113(26),7124-7129(2016)