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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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N413880-1mg
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1mg |
3
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$30.90
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N413880-5mg
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5mg |
3
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$127.90
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N413880-10mg
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10mg |
2
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$216.90
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N413880-25mg
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25mg |
1
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$488.90
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N413880-50mg
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50mg |
1
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$878.90
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N413880-100mg
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100mg |
1
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$1,581.90
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FGFR Inhibitors
| Synonyms | OHKBOEWLASAFLW-DRPHTYIMSA-N | Pregn-5-ene-3,20-diol, 21-(2-hydroxy-1,1,1,3,3,3-hexafluoro-2-propyl)- | 21-(Hydroxy(bistrifluoromethyl)methyl)pregnane-3,20-diol | 4,4,4-trifluoro-1-[(8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,1 |
|---|---|
| Specifications & Purity | ≥98% |
| Biochemical and Physiological Mechanisms | NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. |
| Storage Temp | Store at -20°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
Information NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. Targets FGF3 (Cell-free assay); FGF8b (Cell-free assay); FGF22 (Cell-free assay); FGF20 (Cell-free assay); FGF2/FGFR (Cell-free assay) 16447,15.9 μM(Kd); 18.9 μM(Kd) ;26.8 μM(Kd); 29.4 μM(Kd); 30 μM In vitro NSC12 inhibits FGF-dependent tumor growth, angiogenesis, and metastases. NSC12 does not affect FGF2/heparin interaction, whereas it inhibits the binding of FGF2 to the immobilized receptor (ID50 ∼30 μM). NSC12 interferes with FGF2/FGFR1 interaction without affecting the ability of the growth factor to interact with heparin or HSPGs. NSC12 also binds immobilized FGF3, FGF4, FGF6, FGF8, FGF16, FGF18, FGF20, and FGF22 with Kd values ranging between ∼16 and ∼120 μM. NSC12 may act as a multi-FGF trap by interacting with all members of the canonical FGF subfamilies. NSC12 hampers FGF23-mediated FGFR1 activation in Klotho-expressing Chinese hamster ovary (CHO) cells. Treatment with NSC12 causes the reduction of the S phase of the cell cycle in all tumor cell lines but LLC cells, in which an accumulation in the S phase is observed. NSC12 inhibits FGFR1, FGFR2, FGFR3, and FGFR4 phosphorylation in CHO cell transfectants. NSC12 inhibits the proliferation of various FGF-dependent murine and human cancer cell lines with no inhibitory effect on HCC827 cancer cells that harbor a tumor-driving mutation of the EGFR TK domain and on FGF-independent cancer cell lines. In vivo Parenteral and oral delivery of NSC12 inhibits FGFR activation, tumor growth, angiogenesis, and metastasis in FGF-dependent murine and human tumor models. NSC12 causes a significant decrease of tumor weight, tumor cell FGFR1 phosphorylation and proliferation, and tumor CD31+ neovascularization at all the doses tested in the animal models. Cell Research(from reference) Cell lines:KATO Ⅲ cells Concentrations:1.0 or 3.0 μM Incubation Time:72 h |
| ALogP | 4.884 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 5 |
| Pubchem Sid | 488200702 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488200702 |
| IUPAC Name | 4,4,4-trifluoro-1-[(8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-3-(trifluoromethyl)butane-1,3-diol |
| INCHI | InChI=1S/C24H34F6O3/c1-20-9-7-14(31)11-13(20)3-4-15-16-5-6-18(21(16,2)10-8-17(15)20)19(32)12-22(33,23(25,26)27)24(28,29)30/h3,14-19,31-33H,4-12H2,1-2H3/t14?,15-,16-,17-,18+,19?,20-,21-/m0/s1 |
| InChIKey | OHKBOEWLASAFLW-DRPHTYIMSA-N |
| Smiles | CC12CCC3C(C1CCC2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4C3(CCC(C4)O)C |
| Isomeric SMILES | C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4[C@@]3(CCC(C4)O)C |
| Molecular Weight | 484.52 |
| Reaxy-Rn | 29542218 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29542218&ln= |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 | |
| Certificate of Analysis | Dec 21, 2022 | N413880 |
| Solubility | Solubility (25°C) In vitro Ethanol: 63 mg/mL (130.02 mM); DMSO: 10.3 mg/mL (21.25 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 96 |
| DMSO(mM) Max Solubility | 198.1342359 |
| Water(mg / mL) Max Solubility | <1 |
Starting at $241.90