NSC12 - ≥98% , CAS No.102586-30-1

CAS: 102586-30-1 Cat. No.: N413880 Formula: C₂₄H₃₄F₆O₃ Peso molecolare: 484.52

GRADE & PURITY ≥98%

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

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Panoramica

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 

Specifications

Sinonimi

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

Specifiche e purezza

≥98%

Meccanismi biochimici e fisiologici

NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.

Condizioni di conservazione di stoccaggio

Store at -20°C

Spedito in

Ice chest + Ice pads

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Purezza

≥98%

Proprietà del prodotto

• ALogP: 4.884
• Conteggio HBD: 2
• Legame rotabile: 5

Nomi e identificatori

• Pubchem Sid: 488200702
• Pubchem Sid Url: https://pubchem.ncbi.nlm.nih.gov/substance/488200702
• Sorrisi canonici: CC12CCC3C(C1CCC2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4C3(CCC(C4)O)C
• 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
• InChIKey: OHKBOEWLASAFLW-DRPHTYIMSA-N
• 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
• Isomeri 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
• Peso molecolare: 484.52
• Reaxy-Rn: 29542218
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29542218&ln=

Proprietà chimiche e fisiche

• Solubilità: 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) Solubilità massima: 96
• DMSO (mM) Solubilità massima: 198.1342359
• Acqua (mg/mL) Solubilità massima: ＜1

Domande frequenti

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 102586-30-1, the molecular formula is C24H34F6O3, and the molecular weight is 484.52 g/mol. InChIKey OHKBOEWLASAFLW-DRPHTYIMSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.