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Y15 FAK inhibitor

Name: Y15
Brand: Selleck Chemicals
SKU: S5321
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S5321

Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.

Chemical Structure

Molecular Weight: 284.01

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other FAK Inhibitors	Defactinib (VS-6063) PF-562271 (VS-6062) PF-573228 VS-4718 (PND-1186) PF-562271 HCl PF-562271 Besylate TAE226 (NVP-TAE226) GSK2256098 PF-431396 Ifebemtinib (IN10018, BI-853520)

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (197.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 56 mg/mL

Ethanol : 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.	0.95mg/ml (3.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 19 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.
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.

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	284.01	Formula	C₆H₁₀N₄.4HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	4506-66-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14			Smiles	C1=C(C(=CC(=C1N)N)N)N.Cl.Cl.Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	FAK (Cell-free assay)
In vitro	Y15 treatment in vitro results in decreased cell viability, increased detachment, and increased apoptosis in colon cancer cells, breast cancer cells, and melanoma. In TPC1, BCPAP, K1 and TT cell lines, this compound inhibits pY397 and total FAK expression in a dose-dependent manner. It causes effective dose-dependent detachment in all thyroid cancer cell lines. This chemical causes dose-dependent decrease of colony formation in all papillary thyroid cancer cell lines and increases necrosis in papillary and medullary thyroid cancer cell lines. It does not target homologous Pyk-2, c-Src, c-RAF, EGFR, IGFR, PDGFR, PI3K, VEGFR-3, and c-Met.
In vivo	Y15 blocks breast, pancreatic and neuroblastoma tumor growth in vivo. The pharmacokinetics study in mice demonstrates that, following intraperitoneal administration at 30 mg/kg dose, this compound is very rapidly absorbed in mice, reaching maximum plasma concentration in 4.8 min. It rapidly metabolizes in mouse and human liver microsomes with half-life t_1/2 of 6.9 and 11.6 min, respectively. The maximal tolerated dose of single-dose administration of this chemical by oral administration is 200 mg/kg, and the multiple maximum tolerated dose is 100 mg/kg by PO during 7 day study. It does not cause any mortality or statistically significant differences in the body weight at 30 mg/kg by IP during 28-day study, and at 100 mg/kg by PO during the 7-day study. There are no clinical chemical, hematological, or histopathological changes in different mice organs at 30 mg/kg by IP during 28 days and at 100 mg/kg dose by PO during 7 days.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25277206/ [2] https://academic.oup.com/carcin/article/33/5/1004/2463779 [3] https://pubmed.ncbi.nlm.nih.gov/24915938/

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