ARV-766|CAS 2750830-09-0 |DC Chemicals

Cas No.:	2750830-09-0
Chemical Name:	Luxdegalutamide
Synonyms:	4-[4-[[1-[4-[[[trans-3-(4-Cyano-3-methoxyphenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-N-[(3S)-2,6-dioxo-3-piperidinyl]-2-fluorobenzamide;ARV776;Luxdegalutamide
SMILES:	C(N[C@H]1CCC(=O)NC1=O)(=O)C1=CC=C(N2CCN(CC3CCN(C4=CC=C(C(N[C@@H]5C(C)(C)[C@@H](OC6=CC=C(C#N)C(OC)=C6)C5(C)C)=O)C=C4)CC3)CC2)C=C1F
Formula:	C₄₅H₅₄FN₇O₆
M.Wt:	807.951974391937
Purity:	98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Petrylak D P, et al. A phase 2 expansion study of ARV-766, a PROTAC androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC)[J]. 2023.

Description:	ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].
References:	[1]. Petrylak D P, et al. A phase 2 expansion study of ARV-766, a PROTAC androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC)[J]. 2023.

MSDS

Cat. No.	Product name	Field of application
DC60447	ARV-766	ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].
DC55003	XY028-140 (MS140)	XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).
DC53120	XD2-149	XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.
DC51010	CID 138454799	ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
DC31014	GMB-475	GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein[1].
DC28018	MD-224	MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
DC12022	dBET6	dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.
DC12023	dBET1	dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
DC12380	BSJ-03-123	BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.