For research use only. Not for therapeutic Use.
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].
| Catalog Number | I042959 |
| CAS Number | 1353749-74-2 |
| Synonyms | 2-amino-3-hydroxy-N-[(E)-(2,3,4-trihydroxyphenyl)methylideneamino]propanamide;hydrochloride |
| Molecular Formula | C10H14ClN3O5 |
| Purity | ≥95% |
| 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 |
| 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. |
