PF-6260933

Catalog No.S6499 Batch:S649901

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Technical Data

Formula

C16H13ClN4

Molecular Weight 296.75 CAS No. 1811510-56-1
Solubility (25°C)* In vitro DMSO 59 mg/mL (198.82 mM)
Ethanol 2 mg/mL (6.73 mM)
Water Insoluble
* <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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Biological Activity

Description PF-6260933 (PF-06260933) is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity.
Targets
MAP4K4 [1]
3.7 nM
In vitro

PF-6260933 demonstrates good physicochemical properties as well as moderate human liver microsomal (HLM) clearance[1].

In vivo

Following oral dosing (10 mg/kg), PF-6260933 displays a plasma exposure that provided free drug concentrations above the cell IC50 value for about 4-6 h after administration in a mouse model. PF-6260933 has suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes[1].

Protocol (from reference)

Selleck's PF-6260933 has been cited by 3 publications

Chemical screens in aging-relevant human motor neurons identify MAP4Ks as therapeutic targets for amyotrophic lateral sclerosis [ bioRxiv, 2023, 2023.04.24.538014] PubMed: 37162962
Intestinal epithelial cell-derived exosomes package microRNA-23a-3p alleviate gut damage after ischemia/reperfusion via targeting MAP4K4 [ Biomed Pharmacother, 2022, 149:112810] PubMed: 35303564
Bosutinib prevents vascular leakage by reducing focal adhesion turnover and reinforcing junctional integrity. [ J Cell Sci, 2020, 14;133(9) pii: jcs240077] PubMed: 32198280

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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.