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PRODUCTS SPECIFICATIONS [4506-66-5]
Store
Catalog
SLK-S5321
Brand
Selleck
CAS
4506-66-5
DESCRIPTION [4506-66-5]
Overview
MDL
MFCD00012970
Molecular Weight
284.01
Molecular Formula
C6H10N4.4HCl
SMILES
NC1=C(N)C=C(N)C(N)=C1.Cl
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
3.5210 mL
17.6050 mL
35.2100 mL
5 mM
0.7042 mL
3.5210 mL
7.0420 mL
10 mM
0.3521 mL
1.7605 mL
3.5210 mL
50 mM
0.0704 mL
0.3521 mL
0.7042 mL
Description
Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
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, Y15 inhibits pY397 and total FAK expression in a dose-dependent manner. It causes effective dose-dependent detachment in all thyroid cancer cell lines. Y15 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. Y15 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, Y15 is very rapidly absorbed in mice, reaching maximum plasma concentration in 4.8 min. Y15 rapidly metabolizes in mouse and human liver microsomes with half-life t of 6.9 and 11.6 min, respectively. The maximal tolerated dose of single-dose administration of Y15 by oral administration is 200 mg/kg, and the multiple maximum tolerated dose of Y15 is 100 mg/kg by PO during 7 day study. Y15 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.