CSRM617 hydrochloride

• CAT Number: I042959
• CAS Number: 1353749-74-2
• Molecular Formula: C10H14ClN3O5
• Molecular Weight: 291.69
• Purity: ≥95%
• Synonyms: 2-amino-3-hydroxy-N-[(E)-(2,3,4-trihydroxyphenyl)methylideneamino]propanamide;hydrochloride
• InChI: InChI=1S/C10H13N3O5.ClH/c11-6(4-14)10(18)13-12-3-5-1-2-7(15)9(17)8(5)16;/h1-3,6,14-17H,4,11H2,(H,13,18);1H/b12-3+
• InChIKey: YBUPSOQAGSOATG-QXKVDVGOSA-N
• SMILES: C1=CC(=C(C(=C1C=NNC(=O)C(CO)N)O)O)O.Cl

CSRM617 hydrochloride 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 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model[1]
CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1].
CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1].
CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1].
CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft[1].

Reference

[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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