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CSRM617 hydrochloride

Catalog No. T10896L CAS 1353749-74-2

Synonyms: CSRM617 hydrochloride(787504-88-5 Free base)

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]

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CSRM617 hydrochloride Chemical Structure

CSRM617 hydrochloride, CAS 1353749-74-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
5 mg	In stock	$ 94.00
10 mg	In stock	$ 146.00
25 mg	In stock	$ 282.00
50 mg	In stock	$ 419.00
100 mg	In stock	$ 596.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.47%

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Description	CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 ( OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]
In vitro	CSRM617 hydrochloride, within a concentration range of 0.01-100 μM applied over 48 hours, effectively inhibits the growth of various prostate cancer (PC) cell lines, including PC-3, 22RV1, LNCaP, and C4-2 cells. Furthermore, at concentrations of 10-20 μM over the same duration, it triggers concentration-dependent apoptosis in 22Rv1 cells, evidenced by cell death. Notably, a higher concentration of 20 μM administered for 72 hours leads to apoptosis in 22Rv1 cells, marked by the presence of cleaved Caspase-3 and PARP.
In vivo	CSRM617, administered orally at a dosage of 50 mg/kg daily for 20 days, significantly inhibits tumor growth in SCID mice with 22Rv1 xenografts. This regimen was observed to notably impede the development and proliferation of diffuse metastases in the tested animal model.

Synonyms	CSRM617 hydrochloride(787504-88-5 Free base)
Molecular Weight	291.69
Formula	C10H14ClN3O5
CAS No.	1353749-74-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (154.27 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

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