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Chemical Structure : Pz-1
Catalog No.: PC-61163Not For Human Use, Lab Use Only.
A potent, dual pan-RET/VEGFR2 kinase inhibitor with IC50s of <1 nM for all RET, RET V804M and VEGFR2.
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A potent, dual pan-RET/VEGFR2 kinase inhibitor with IC50s of <1 nM for all RET, RET V804M and VEGFR2; displays good global kinase selectivity with only 7 kinases against a 91 kinase panel at 50 nM, strongly inhibites phosphorylation of RET and mutant RET oncoproteins at 1 nM in cell-based assays, inhibits RETC634Y NIH3T3 fibroblast proliferation with IC50 of 0.5 nM; abrogates the formation of tumors induced by RET-mutant fibroblasts and blocks the phosphorylation of both RET and VEGFR2 in tumor tissue at 1.0 mg/kg without detectable toxicity.
| M.Wt | 454.534 | |
| Formula | C26H26N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Frett B, et al. Angew Chem Int Ed Engl. 2015 Jul 20;54(30):8717-21.
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