Molecular Formula | C6H11ClN4 |
Molar Mass | 174.63 |
Density | 1.401g/cm3 |
Melting Point | ≥300°C(lit.) |
Boling Point | 400.9°C at 760 mmHg |
Flash Point | 233.6°C |
Solubility | H2O: soluble20mg/mL, clear |
Vapor Presure | 1.23E-06mmHg at 25°C |
Appearance | powder |
Color | , faint purple to dark brown |
BRN | 3701344 |
Storage Condition | room temp |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month. |
Refractive Index | 1.827 |
In vitro study | Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 μM in Panc-1 cells. At a dose of 100 μM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC 50 is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively. |
In vivo study | Nude mice bearing Panc si-ctrl xenografts are treated with TAE226, a dual FAK and IGF-1R tyrosine kinase inhibitor, to provide a reference for the antitumor effect of dual inhibition of FAK and IGF-1R. Without drug treatment, Panc si5-IGF-1R xenografts grew slower than Panc si-ctrl xenografts (Panc si5-IGF-1R/PBS vs. Panc si-ctrl/PBS), suggesting moderate tumor suppression by inhibiting the IGF-1R pathway only. Further inhibition of FAK activity by Y15 treatment suppresses the growth of Panc si5-IGF-1R xenografts more drastically (Panc si5-IGF-1R/PBS vs. Panc si5-IGF-1R/Y15). A similar antitumor effect is seen in Panc si-ctrl xenografts treated with TAE226 (Panc si5-IGF-1R/Y15 vs. Panc si-ctrl/TAE226). Mice demonstrates normal grooming and eating habits throughout the experiment. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
FLUKA BRAND F CODES | 10 |
Use | 1,2,4, 5-phenyltetramine tetrahydrochloride directly blocks the phosphorylation of focal adhesion kinase (FAK) in a dose-and time-dependent manner, and also shows breast tumor regression in vivo. Targeting the Y397 site of FAK with FAK inhibitor 14 has been proposed to be effective for cancer therapy. |
application | 1,2,4, 5-phenyltetramine tetrahydrochloride light purple powder, used for synthetic material intermediates and pharmaceutical research and development intermediates, can be used in laboratory research and development and chemical medicine synthesis process. |
biological activity | Y15 is an effective and specific focal adhesion kinase inhibitor (FAK), which can inhibit its autophosphorylation activity, reduce the vitality of cancer cells and block tumor growth. |
Target | Value |