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
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.81mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.9mg/ml Taking the 1 mL working solution as an example, add 50 μL of 98 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.