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Technical Data
| Formula | C31H33FN6O3 |
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| Molecular Weight | 556.63 | CAS No. | 945614-12-0 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (179.65 mM) | |
| Ethanol | 100 mg/mL (179.65 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Pexmetinib is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1. | ||
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| Targets |
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| In vitro | In HeLa cells, Pexmetinib inhibits phospho-HSP27 with IC50 of 2 nM. In isolated PBMCs and human whole blood cells, Pexmetinib inhibits LPS-Induced TNFα with IC50 of 4.5 nM and 313 nM, respectively. [1] | ||
| In vivo | In male Swiss Webster mice, Pexmetinib (30 mg/kg, p.o.) inhibits the production of the proinfl ammatory cytokines TNFα and IL6 in response to lipopolysaccharide (LPS) or staphyloccus enterotoxin A. In established RPMI 8226 xenografts, ARRY-614 (25 mg/kg, p.o.) inhibits tumor growth and shows additive activity when combines with thalidomide. In ovarian carcinoma A2780 xenografts, ARRY-614 (30 mg/kg, p.o.) also shows additive tumor growth inhibition activity when combines with Taxol. [1] |
Protocol (from reference)
| Animal Study: |
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References
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Selleck's Pexmetinib has been cited by 4 publications
| Pexmetinib suppresses osteoclast formation and breast cancer induced osteolysis via P38/STAT3 signal pathway [ J Bone Oncol, 2022, 35:100439] | PubMed: 35800294 |
| Metastatic colorectal cancer cells maintain the TGFβ program and use TGFBI to fuel angiogenesis [ Theranostics, 2021, 11(4):1626-1640] | PubMed: 33408771 |
| MAGI1 inhibits the AMOTL2/p38 stress pathway and prevents luminal breast tumorigenesis [ Sci Rep, 2021, 11(1):5752] | PubMed: 33707576 |
| Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [ J Pharmacol Exp Ther, 2019, 370(2):219-230] | PubMed: 31189728 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.