[CAS NO. 4506-66-5]  Y15

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PRODUCTS SPECIFICATIONS [4506-66-5]

Store
Catalog
SLK-S5321
Brand
Selleck
CAS
4506-66-5

DESCRIPTION [4506-66-5]

Overview

MDLMFCD00012970
Molecular Weight284.01
Molecular FormulaC6H10N4.4HCl
SMILESNC1=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 mg5 mg10 mg
1 mM3.5210 mL17.6050 mL35.2100 mL
5 mM0.7042 mL3.5210 mL7.0420 mL
10 mM0.3521 mL1.7605 mL3.5210 mL
50 mM0.0704 mL0.3521 mL0.7042 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.

Targets

FAK [1]
(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, 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.


Synonyms

1,2,4,5-Benzenetetramine, hydrochloride (1:4)
1,2,4,5-Benzenetetramine, tetrahydrochloride
1,2,4,5-Tetraaminobenzene tetrahydrochloride
FAK Inhibitor 14
NSC 667249
Y 15
NSC 677249