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CSRM617 hydrochloride

🥰Excellent
Catalog No. T10896LCas No. 1353749-74-2
Alias 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 Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

CSRM617 hydrochloride

CSRM617 hydrochloride

🥰Excellent
Purity: 99.47%
Catalog No. T10896LAlias CSRM617 hydrochloride(787504-88-5 Free base)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. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].
Pack SizePriceAvailabilityQuantity
5 mg$56In Stock
10 mg$87In Stock
25 mg$169In Stock
50 mg$251In Stock
100 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Purity:99.47%
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Product Introduction

Bioactivity
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. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and 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.
AliasCSRM617 hydrochloride(787504-88-5 Free base)
Chemical Properties
Molecular Weight291.69
FormulaC10H14ClN3O5
Cas No.1353749-74-2
SmilesCl.NC(CO)C(=O)N\N=C\c1ccc(O)c(O)c1O
Relative Density.1.68 g/cm3 at 21℃
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (154.27 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.4283 mL17.1415 mL34.2830 mL171.4149 mL
5 mM0.6857 mL3.4283 mL6.8566 mL34.2830 mL
10 mM0.3428 mL1.7141 mL3.4283 mL17.1415 mL
20 mM0.1714 mL0.8571 mL1.7141 mL8.5707 mL
50 mM0.0686 mL0.3428 mL0.6857 mL3.4283 mL
100 mM0.0343 mL0.1714 mL0.3428 mL1.7141 mL

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