CSRM617 hydrochloride( —— )

Catalog No. M32871 CAS No. 1353749-74-2

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 μM in SPR assays, directly binding to the OC2-HOX domain.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

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Biological Information

Product Name

CSRM617 hydrochloride
Note

Research use only, not for human use.
Brief Description

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 μM in SPR assays, directly binding to the OC2-HOX domain.
Description

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
In Vitro

CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells.CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion.CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP.
In Vivo

CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft.Animal Model:SCID mice with 22Rv1 xenograft Dosage:50 mg/kg Administration:Oral administration; daily, for 20 days Result:Elicited a significant reduction in the onset and growth of diffuse metastases.
Synonyms

——
Pathway

Apoptosis
Target

Apoptosis
Recptor

Apoptosis | Androgen Receptor
Research Area

——
Indication

——

Chemical Information

CAS Number

1353749-74-2
Formula Weight

291.69
Molecular Formula

C10H14ClN3O5
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 125 mg/mL (428.54 mM; Ultrasonic )
SMILES

Cl.NC(CO)C(=O)N\N=C\c1ccc(O)c(O)c1O
Chemical Name

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

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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