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10-4802

MTX-531

Size

£182.00

SKU:
10-4802
Physical State:
Solid
Molecular Weight:
453.95
Purity:
>98%
Purification:
HPLC Purified
Storage Conditions:
-20[o]C
Supplier:
Focus Biomolecules
CAS Number:
2791417-66-6
Immunogen:
Kinase
Extra Details:
MTX-531 is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM; PI3kA Alpha = 6.4 nM; PI3KB Beta = 233 nM; PI3KG Gamma = 8.3 nM; PI3KD Delta = 1.1 nM; mTOR = 105 nM; DNA-PK = 5.4 nM). MTX-531 displayed exquisite selectivity for EGFR and PI3K family members (against >400 protein/lipid kinases). It displayed efficacy in the treatment of head and neck squamous cell carcinomas and in combination with RAS inhibitors in BRAF-mutant and KRAS-mutant colorectal and pancreatic cancers. Additionally, it did not produce a hyperglycemic response that is typical for PI3K inhibitors. An interesting new chemical tool for cancer research that targets two key resistance drivers.
Shipping Conditions:
Ambient