1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

IDH1 Inhibitor 1 

Cat. No.: HY-112601
Handling Instructions

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.

For research use only. We do not sell to patients.

IDH1 Inhibitor 1 Chemical Structure

IDH1 Inhibitor 1 Chemical Structure

CAS No. : 2234285-81-3

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1].

IC50 & Target

IC50: 0.021 μM (IDH1R132H), 0.045 μM (IDH1R132C), and 2.52 μM (IDH1WT)[1]

In Vitro

IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM[1].

In Vivo

IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2203 mL 11.1015 mL 22.2030 mL
5 mM 0.4441 mL 2.2203 mL 4.4406 mL
10 mM 0.2220 mL 1.1101 mL 2.2203 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

450.39

Formula

C₂₀H₁₈F₄N₆O₂

CAS No.

2234285-81-3

SMILES

C[[email protected]](NC1=NC(N2[[email protected]@H](CF)COC2=O)=CC=N1)C(N=C3)=CN3C4=CC=C(C(F)(F)F)C=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
IDH1 Inhibitor 1
Cat. No.:
HY-112601
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IDH1 Inhibitor 1

Cat. No.: HY-112601