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Cayman ARV-771
List Price $63.00 Your Price $63.00
Cayman ARV-771 - CAYM (Additional S&H Or Hazmat Fees May Apply)
NETA PART: CAYM-21299-1
MFG.PART: 21299-1
UNSPSC: 12352200
Manufacturer: Cayman
Product Description
ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins. It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.
WARNING This product is not for human or veterinary use.
Technical Information
Formal Name
(2S,4R)-1-((S)-
CAS Number
1949837-12-0
Molecular Formula
C49H60ClN9O7S2
Formula Weight
986.6
Purity
≥95%
Formulation
A crystalline solid
Solubility
- DMF: 20 mg/mL
- DMF:PBS (pH 7.2) (1:6): 0.14 mg/mL
- DMSO: 15 mg/mL
- Ethanol: 10 mg/mL
λmax
257 nm
SMILES
CC1=NN=C2[C@H](CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N3C[C@H](O)C[C@H]3C(N[C@@H](C)C4=CC=C(C5=C(C)N=CS5)C=C4)=O)=O)=O)=O)N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N21
InChi Code
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(13-11-32)43-29(3)52-26-67-43/h10-17,26
InChi Key
PQOGZKGXGLHDGS-QQRWPDCKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room Temperature in continental US; may vary elsewhere
Stability
≥ 4 years
| SKU | CAYM-21299-1 |
|---|---|
| Supplier Part Number | 21299-1 |
| UM | EA |
| UNSPSC | 12352200 |
| Manufacturer | Cayman |
| MSDS URL | Click here |
| Temperature | -20 |
| Refrigerated-Frozen | Y |
| CountryOfOrigin | China |
| ProductLine | CAYM |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 5 |
| Hazardous | N |
| CAS Number | 1949837-12-0 |
| Energy Star | No |
| Green | No |
| Controlled | N |