Description
ARV-771 | B3368
Description: ARV-771 is a potent BET bromodomain PROTAC® degrader with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. Degrades BRD2/3/4 in castration-resistant prostate cancer (CRPC) cell lines. Reduces androgen receptor levels and induces apoptosis in CRPC cells in vitro. Down-regulates BRD4 and induces tumor regression in CRPC xenografts in mice. Also reduces leukemia burden in a mouse model. Induces degradation of BRD-tagged CAR (chimeric antigen receptor) in T cells.
Alternate Name/Synonyms: (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-carboxamide
Appearance: Off-white solid
Formulation:
CAS Number: 1949837-12-0
Strcture Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₄₉H₆₀ClN₉O₇S₂
Molecular Weight: 986.65
Cell-Permeable?: True
Purity: ≥98% by HPLC
Solubilities: >60 mg/ml DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Tag Line: A potent BET bromodomain PROTAC®
MDL Number:
PubChem CID: 126619980
PubChem CID Link: https://pubchem.ncbi.nlm.nih.gov/compound/126619980
SMILES: CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NC(C)C5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)C7=CC=C(C=C7)Cl)C
InChi: InChI=1S/C49H60ClN9O7S2/c1-27-30(4)68-48-41(27)42(33-14-16-35(50)17-15-33)54-37(45-57-56-31(5)59(45)48)23-39(61)51-18-21-65-19-9-20-66-25-40(62)55-44(49(6,7)8)47(64)58-24-36(60)22-38(58)46(63)53-28(2)32-10-12-34(12-26-67-43/h10-17,26,28,36-38,44,60H,9,18-25H2,1-8H3,(H,51,61)(H,53,63)(H,55,62)/t28-,36+,37-,38-,44+/m0/s1
InChi Key: PQOGZKGXGLHDGS-QQRWPDCKSA-N
Category: Biochemicals
Additional Information
Storage Conditions: |
-20ºC |
Shipping Conditions: |
Gel Pack |
Shelf life: |
36month |