IDH-305

Catalog No.S3574 Batch:S357401

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Technical Data

Formula

C23H22F4N6O2
Molecular Weight 490.45 CAS No. 1628805-46-8
Solubility (25°C)* In vitro DMSO 98 mg/mL (199.81 mM)
Ethanol 98 mg/mL (199.81 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.)

Preparing Stock Solutions

Biological Activity

Description IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
Targets
IDH1R132H [1]
(Cell-free assay)		 IDH1R132C [1]
(Cell-free assay)		 IDH1WT [1]
(Cell-free assay)
27 nM 28 nM 6.14 μM
In vitro

IDH-305 inhibits HCT116-IDH1R132H/+ cells with an IC50 of 24 nM.[1]
In vivo

IDH-305 exhibits in vivo correlation of 2-HG reduction and efficacy in a patient-derived IDH1 mutant xenograft tumor model.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MCF10A-IDH1R132H/+

  • Concentrations

    0.001-10 μM

  • Incubation Time

    --

  • Method

    --
Animal Study:

[1]
  • Animal Models

    Nu/nu mice of HMEX2838-IDH1R132C+/- PDX model

  • Dosages

    30, 100, 300 mg/kg

  • Administration

    p.o.

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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.