Name: NSC12
Brand: Selleck Chemicals
SKU: S7940
Availability: InStock
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Batch: S794001 Ethanol]63 mg/mL]false]DMSO]10.3 mg/mL]false]Water]Insoluble]false Purity: 99.91%

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COA
NMR
HPLC
SDS
Datasheet

99.91

Related Targets	EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl
Other FGFR Inhibitors	PD173074 Fexagratinib (AZD4547) BLU9931 LY2874455 Zoligratinib (Debio-1347) Futibatinib (TAS-120) PD-166866 SSR128129E H3B-6527 Fisogatinib (BLU-554)

Solubility

In vitro
Batch:

Ethanol : 63 mg/mL

DMSO : 10.3 mg/mL (21.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	484.52	Formula	C₂₄H₃₄F₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	102586-30-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 172285			Smiles	CC12CCC3C(C1CCC2C(CC(C(F)(F)F)(C(F)(F)F)O)O)CC=C4C3(CCC(C4)O)C

Mechanism of Action

Targets/IC₅₀/Ki	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 FGF2 (Cell-free assay) 51 μM(Kd) FGF16 (Cell-free assay) 53.7 μM(Kd) FGF6 (Cell-free assay) 53.8 μM(Kd) FGF18 (Cell-free assay) 63.4 μM(Kd) FGF4 (Cell-free assay) 119 μM(Kd)
In vitro	NSC12 inhibits FGF-dependent tumor growth, angiogenesis, and metastases. This compound does not affect FGF2/heparin interaction, whereas it inhibits the binding of FGF2 to the immobilized receptor (ID50 ∼30 μM). It interferes with FGF2/FGFR1 interaction without affecting the ability of the growth factor to interact with heparin or HSPGs. This chemical also binds immobilized FGF3, FGF4, FGF6, FGF8, FGF16, FGF18, FGF20, and FGF22 with Kd values ranging between ∼16 and ∼120 μM. It may act as a multi-FGF trap by interacting with all members of the canonical FGF subfamilies. This compound hampers FGF23-mediated FGFR1 activation in Klotho-expressing Chinese hamster ovary (CHO) cells. Treatment with it 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. It inhibits FGFR1, FGFR2, FGFR3, and FGFR4 phosphorylation in CHO cell transfectants. This inhibitor reduces 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. This compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26267536/

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NSC12 FGFR inhibitor

Chemical Structure

Molecular Weight: 484.52