TPX-0046

Catalog No.S9826 Batch:S982602

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Technical Data

Formula

C21H21FN6O3
Molecular Weight 424.43 CAS No. 2359650-19-2
Solubility (25°C)* In vitro DMSO 2 mg/mL (4.71 mM)
Water Insoluble
Ethanol 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

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.
Targets
RET [1] SRC [1]
In vitro

TPX-0046 is a new type of RET/SRC inhibitor and potent against a range of RET fusions and mutations including solvent front mutations (SFMs)-mediated resistance. In Ba/F3 RET engineered cells with SFMs proliferation test, the average IC50 is 1-17 nM.[2]
In vivo

TPX-0046 demonstrates marked anti-tumor efficacy in vivo in multiple RET-driven cancer cell-derived and patient-derived xenograft tumor models.[2]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Ba/F3 RET engineered cells with SFMs, KIF5B-RET Ba/F3, LC2/ad, and TT cells

  • Concentrations

    --

  • Incubation Time

    --

  • Method

    Cell proliferation assays
Animal Study:

[2]
  • Animal Models

    Ba/F3 KIF5B-RET xenograft model

  • Dosages

    5 mg/kg

  • Administration

    --

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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.