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GW280264X

Cat. No. M10630
GW280264X Structure
Synonym:

GW-280264

Size Price Availability Quantity
5mg USD 450  USD450 In stock
10mg USD 820  USD820 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

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 575.72
Formula C28H41N5O6S
CAS Number 866924-39-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

[1] Nina Hedemann, et al. Cancers (Basel) . ADAM17 Inhibition Increases the Impact of Cisplatin Treatment in Ovarian Cancer Spheroids

[2] Indrani Dutta, et al. Cancer Lett . ADAM protease inhibition overcomes resistance of breast cancer stem-like cells to γδ T cell immunotherapy

[3] Jinling Yang, et al. J Biol Chem. ADAM10 and ADAM17 proteases mediate proinflammatory cytokine-induced and constitutive cleavage of endomucin from the endothelial surface

[4] Charles J Malemud. Biochem Pharmacol . Inhibition of MMPs and ADAM/ADAMTS

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GW280264X, GW-280264 supplier, inhibitors

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