GW280264X is an ADAM17 inhibitor. GW280264X (ADAMi), an inhibitor of both ADAM10 and ADAM17, significantly increased surface MICA/B on both SUM149 and PDX401 cells. GW280264X blocked MICA shedding, which lead to significantly enhanced γδTc cytotoxicity against BCSC. Using GW280264X in combination with γδΤc also increased cytotoxicity against NSC, this approach could be considered to generally enhance γδTc targeting of cancer types using MICA shedding as an immune evasion mechanism.
| Molecular Weight | 575.72 |
| Formula | C28H41N5O6S |
| CAS Number | 866924-39-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[4] Charles J Malemud. Biochem Pharmacol . Inhibition of MMPs and ADAM/ADAMTS
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