102586-30-1

Basic information

• Product Name: NSC-12
• Synonyms: CS-2338;CS-2161;NSC172285;NSC12，NSC 172285;NSC-12;NSC 12;NSC12;21-Norchol-5-ene-3,20,23-triol, 24,24,24-trifluoro-23-(trifluoromethyl)-, (3β,20S)-
• CAS NO: 102586-30-1
• Molecular Formula: C24H34F6O3
• Molecular Weight: 484.5153792
• EINECS: -0
• Mol File: 102586-30-1.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 521.8±45.0 °C(Predicted)
• Appearance: /
• Density: 1.31±0.1 g/cm3(Predicted)
• PKA: 9.50±0.29(Predicted)
• CAS DataBase Reference: NSC-12(CAS DataBase Reference)
• NIST Chemistry Reference: NSC-12(102586-30-1)
• EPA Substance Registry System: NSC-12(102586-30-1)

Safety Data

• Hazardous Substances Data: 102586-30-1(Hazardous Substances Data)

Usage

General Description

NSC-12 is a novel and potent small-molecule inhibitor of the cell cycle checkpoint kinase 1 (Chk1) and has shown promising results in preclinical studies as a potential cancer treatment. It has been shown to exhibit strong anti-proliferative and cytotoxic effects in a wide range of cancer cell lines, including those resistant to traditional chemotherapy. NSC-12 has also been reported to enhance the efficacy of DNA-damaging agents, suggesting its potential use in combination therapy for cancer treatment. Additionally, it has demonstrated good pharmacokinetic properties and tolerability in animal models, making it a promising candidate for further development as a targeted therapy for cancer.

Upstream product

• 1639-44-7 3β-hydroxy-21-carboxy-pregn-5-en-20-ol 
• 145-13-1 Pregnenolone 
• 1778-02-5 Pregnenolone acetate 

Relevant articles and documents

Synthesis, Structural Elucidation, and Biological Evaluation of NSC12, an Orally Available Fibroblast Growth Factor (FGF) Ligand Trap for the Treatment of FGF-Dependent Lung Tumors

NSC12 is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. It was identified by virtual screening from a NCI small molecule library, but no data were available about its synthesis, stereochemistry, and physicochemical properties. We report here a synthetic route that allowed us to characterize and unambiguously identify the structure of the active compound by a combination of NMR spectroscopy and in silico conformational analysis. The synthetic protocol allowed us to sustain experiments aimed at assessing its therapeutic potential for the treatment of FGF-dependent lung cancers. A crucial step in the synthesis generated a couple of diastereoisomers, with only one able to act as a FGF trap molecule and to inhibit FGF-dependent receptor activation, cell proliferation, and tumor growth when tested in vitro and in vivo on murine and human lung cancer cells.