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:
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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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