MTX-531 | Dual EGFR/PI3K inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $85.00 | ||
| 25 mg | $315.00 |
MTX-531 (2791417-66-6) is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM; PI3kα = 6.4 nM; PI3Kß = 233 nM; PI3Kγ = 8.3 nM; PI3Kδ = 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.
References/Citations:
- Whitehead et al. (2024), A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance Nat. Cancer 5 1250
C22H20ClN5O2S
>98% HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
MTX-531 (2791417-66-6) is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM; PI3kα = 6.4 nM; PI3Kß = 233 nM; PI3Kγ = 8.3 nM; PI3Kδ = 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.
References/Citations:
- Whitehead et al. (2024), A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance Nat. Cancer 5 1250
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