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Chemical Structure : Pexmetinib
Catalog No.: PC-35149Not For Human Use, Lab Use Only.
Pexmetinib (ARRY-614) is a potent, orally active, dual Tie-2/p38 MAPK inhibitor with IC50 of 1, 26 and 35 nM for Tie-2, p38α and p38β, respectively.
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Pexmetinib (ARRY-614) is a potent, orally active, dual Tie-2/p38 MAPK inhibitor with IC50 of 1, 26 and 35 nM for Tie-2, p38α and p38β, respectively; demonstrates in vitro mechanistic models (Angpt-1 or anisomycin-stimulated HUVEC) as well as functional readouts (LPS-induced TNF-alpha release from human PBMCs) with IC50 of 2282 nM and 172 nM for Tie2 and p38, respectively; abrogates cytokine mediated myelosuppresive effects in hematopoietic cells; inhibits leukemic cell proliferation and stimulates hematopoietic activity in MDS; inhibits LPS-induced TNF-alpha release) murine models .
Blood Cancer
Phase 1 Discontinued
| M.Wt | 556.63 | |
| Formula | C31H33FN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bachegowda L, et al. Cancer Res. 2016 Aug 15;76(16):4841-4849.
2. Garcia-Manero G, et al. Clin Cancer Res. 2015 Mar 1;21(5):985-94.
3. Wollenberg LA, et al. Clin Pharmacol. 2015 Sep 30;7:87-95.
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