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Y15

Cat. No. M5347
Y15 Structure
Synonym:

FAK inhibitor Y15; FAK Inhibitor 14

Size Price Availability Quantity
10mM*1mL USD 55  USD55 In stock
10mg USD 45  USD45 In stock
50mg USD 95  USD95 In stock
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Quality Control
Biological Activity

In vitro: directly inhibited FAK autophosphorylation in a dose- and time-dependent manner. Furthermore, Y15 increased pancreatic cancer cell detachment and inhibited cell adhesion in a dose-dependent manner. Inhibition of FAK pathway using Y15 significantly decreased cell survival, adhesion, and promoted apoptosis. Y15 significantly decreased viability and clonogenicity in a dose-dependent manner, increased detachment in a dose- and time-dependent manner, caused apoptosis, and inhibited cell invasion in both cell lines. In addition, Y15 treatment decreased autophosphorylation of FAK in a dose-dependent manner and changed cell morphology by causing cell rounding in DBTRG and U87 cells. In vivo: Y15 effectively caused human pancreatic tumor regression in vivo, when administered alone and its effects were synergistic with gemcitabine chemotherapy. The combination of Y15 treatment and IGF-1R knockdown also showed significant antitumor effect in vivo. Y15 was administered in an orthotopic glioma model, leading to an increase in mouse survival.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 284.01
Formula C6H14Cl4N4
CAS Number 4506-66-5
Purity >98%
Solubility 10mM in DMSO
Storage at -20°C
References

[1] Golubovskaya V, et al. J Cancer Res Clin Oncol. Down-regulation of ALDH1A3, CD44 or MDR1 sensitizes resistant cancer cells to FAK autophosphorylation inhibitor Y15.

[2] Golubovskaya V, et al. Arch Toxicol. In vivo toxicity, metabolism and pharmacokinetic properties of FAK inhibitor 14 or Y15 (1, 2, 4, 5-benzenetetramine tetrahydrochloride).

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Y15, FAK inhibitor Y15; FAK Inhibitor 14 supplier, FAK, inhibitors

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