Y15 hydrochloride

• CAS: 4506-66-5
• Catalog Number: ACM4506665
• Category: Inhibitors
• Molecular Weight: 284.01
• Molecular Formula: C6H14Cl4N4
• Description: Y15 hydrochloride, also known as FAK Inhibitor 14, is a direct FAK autophosphorylation inhibitor, blocking phosphorylation of Y397 with an IC50 value of about 1 μM. Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Y15 was shown to decrease cancer growth in vitro and in vivo.
• Synonyms: Y15 hydrochloride; Y15 tetrahydrochloride; Y 15; Y-15. FAK Inhibitor 14
• IUPAC Name: 1,2,4,5-benzenetetramine tetrahydrochloride
• Canonical SMILES: NC1=CC(N)=C(N)C=C1N.[H]Cl.[H]Cl.[H]Cl.[H]Cl
• InChI: InChI=1S/C6H10N4.4ClH/c7-3-1-4(8)6(10)2-5(3)9;;;;/h1-2H,7-10H2;4*1H
• InChI Key: BZDGCIJWPWHAOF-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Light green to green solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: Y15 is an inhibitor of focal adhesion kinase (FAK).
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 25.37; H, 4.97; Cl, 49.93; N, 19.73
• HS Tariff Code: 292159
• In Vitro Activity: In each cell line Y15 inhibited pY397 and total FAK expression in a dose-dependent manner. TT was the most sensitive cell line with effective inhibition of pY397 expression by 3 μM Y15 (Figure 2A). TPC1 cells had inhibition of phosphorylated FAK and total FAK expression at 30 μM Y15 (Figure 2B). K1 had Y397-FAK and FAK inhibition at 50 μM (Figure 2C) and BCPAP had inhibition of pY397 and FAK expression levels at 40 μM Y15 (Figure 2D). Thus, Y15 decreased pY397 and total FAK levels in a dose-dependent manner, most in the medullary thyroid cancer cell line and to a lesser extent in the papillary thyroid cancer cell lines.; Reference: Oncotarget. 2014 Sep; 5(17): 7945-7959. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4202172/
• In Vivo Activity: Although weight-loss was similar in both infected groups [Fig. 2B], three doses of Y15 were sufficient to significantly extend survival time by 3 days and increase survival [Fig. 2C]. Importantly, DMSO-treated mice either succumbed to the infection (4/8) or were euthanized based on reaching symptom end-points before reaching body weight-loss cut-off. In contrast, most (7/8) Y15-treated mice were euthanized due to reaching body weight-loss cut-off with mild symptoms being observed. These data indicate that short-term prophylactic intranasal administration of Y15 results in prolonged survival of an extremely susceptible host.; Reference: Virology. 2019 Aug;534:54-63. https://pubmed.ncbi.nlm.nih.gov/31176924/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).