Elzovantinib (TPX-0022)

Catalog No.S9620 Batch:S962001

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Technical Data

Formula

C20H20FN7O2

Molecular Weight 409.42 CAS No. 2271119-26-5
Solubility (25°C)* In vitro Ethanol 5 mg/mL (12.21 mM)
DMSO Insoluble
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.)

Preparing Stock Solutions

Biological Activity

Description Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
Targets
SRC [1]
(Cell-free assay)
MET [1]
(Cell-free assay)
CSF1R [1]
(Cell-free assay)
0.12 nM 0.14 nM 0.71 nM
In vitro

In a Ba/F3 ETV6-CSF1R cell model, TPX-0022 inhibits both autophosphorylation of CSF1R with an IC50 <3 nM and cell growth with an IC50 of 14 nM, thus effectively inhibits tumor growth .<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

TPX-0022 effectively inhibits the growth of Ba/F3 ETV6-CSF1R xenograft tumors in vivo.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

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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.

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