| Identification | Back Directory | [Name]
NSC-12 | [CAS]
102586-30-1 | [Synonyms]
CS-2161
CS-2338
NSC-12;NSC 12;NSC12
21-Norchol-5-ene-3,20,23-triol, 24,24,24-trifluoro-23-(trifluoromethyl)-, (3β,20S)- | [Molecular Formula]
C24H34F6O3 | [MDL Number]
MFCD31544308 | [MOL File]
102586-30-1.mol | [Molecular Weight]
484.52 |
| Chemical Properties | Back Directory | [Boiling point ]
521.8±45.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 2 mg/ml; DMSO: 0.1 mg/ml; Ethanol: 20 mg/ml; Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml | [form ]
A crystalline solid | [pka]
9.50±0.29(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
NSC 12 is an extracellular trap of fibroblast growth factor 2 (FGF2) that binds FGF2 and interferes with its interaction with FGFR1. NSC12 inhibits the proliferation of different FGF-dependent tumour cells both in vitro and in vivo with no systemic toxic effects[1]. | [Biological Activity]
NSC12 (NSC 172285) is an orally available inhibitor of FGF2/FGFR interaction with potential antitumor activity. | [in vitro]
NSC-12 can inhibit FGF-dependent tumor growth, angiogenesis and metastasis. It did not affect FGF2/heparin interaction, but inhibited FGF2 binding to immobilized receptors (IC50 ~30 μM), it disrupted FGF2 interaction with FGFR1, and had no effect on the interaction activity of growth factors with heparin or HSPGs . | [in vivo]
Administered by injection and oral route, NSC-12 inhibits FGFR activation, tumor growth, angiogenesis and metastasis in FGF-dependent mouse and human tumor models. In animal models, it significantly reduced tumor weight, tumor cell FGFR1 phosphorylation levels and proliferation, and tumor CD31+ cardiovascular formation. | [target]
| Target | Value | FGF3
(Cell-free assay) | 15.9 μM(Kd) | FGF8b
(Cell-free assay) | 18.9 μM(Kd) | FGF22
(Cell-free assay) | 26.8 μM(Kd) | FGF20
(Cell-free assay) | 29.4 μM(Kd) | FGF2/FGFR
(Cell-free assay) | 30 μM |
| [storage]
Store at -20°C | [References]
[1] Ronca R, et al. Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy. Cancer Cell. 2015 Aug 10;28(2):225-39. DOI:10.1016/j.ccell.2015.07.002 |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|