787504-88-5

787504-88-5 structure

Name: CSRM617
Chemical Name: CSRM617
CAS Number: 787504-88-5
Molecular Formula: C₁₀H₁₃N₃O₅
Molecular Weight: 255.23
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2019-11-04 19:55:49
Modify Date: 2024-01-22 00:24:23
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model[1]

Name	CSRM617

Description	CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model[1]
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Others >> Androgen Receptor
In Vitro	CSRM617 (0.01-100 μM; 48 hours) inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1]. CSRM617 (10-20 μM; 48 hours) induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1]. CSRM617 (20 μM; 72 hours) induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1].
References	[1]. Rotinen M, et al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898.

Molecular Formula	C₁₀H₁₃N₃O₅
Molecular Weight	255.23