CSRM617|CSRM-617;CSRM 617|DC Chemicals

Cas No.:	787504-88-5
Chemical Name:	2-amino-3-hydroxy-N'-(2,3,4-trihydroxybenzylidene)propanehydrazide
Synonyms:	CSRM-617;CSRM 617
SMILES:	C(N/N=C/C1=CC=C(O)C(O)=C1O)(=O)C(N)CO
Formula:	C₁₀H₁₃N₃O₅
M.Wt:	255.23
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

Description:	CSRM617 (CSRM-617) is a small-molecule inhibitor of the transcription factor ONECUT2 (OC2) with Kd of 7.43 uM in SPR assays, binds to OC2-HOX domain directly; inhibits cell growth and induced apoptosis in vitro in several PC cell lines that expressed moderate to high levels of OC2; significantly downregulates PEG10 protein levels in tumors from mice treated with CSRM617, suppresseses metastasis in 22Rv1 cells implanted subcutaneously nude mice.
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.

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