1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. IDH-305

IDH-305 

Cat. No.: HY-104036 Purity: 98.75%
Handling Instructions

IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT)).

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

IDH-305 Chemical Structure

IDH-305 Chemical Structure

CAS No. : 1628805-46-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 363 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 363 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 336 In-stock
Estimated Time of Arrival: December 31
10 mg USD 576 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
200 mg USD 3480 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT))[1][2].

IC50 & Target

IC50: 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT)[1]

In Vitro

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

IDH-305 (30-300 mg/kg; p.o.; twice daily for 21 days) inhibits 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: nu/nu mice (HMEX2838-IDH1R132C+/-PDX model)[1]
Dosage: 30, 100, 300 mg/kg
Administration: Oral gavage; twice daily for 21 days
Result: Resulted in 62-67% 2-HG reduction and significant anti-tumor activity at 100 mg/kg and 97-99% 2-HG reduction and partial tumor regression of 32% at 300 mg/kg.
Clinical Trial
Molecular Weight

490.45

Formula

C₂₃H₂₂F₄N₆O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (305.84 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0389 mL 10.1947 mL 20.3894 mL
5 mM 0.4078 mL 2.0389 mL 4.0779 mL
10 mM 0.2039 mL 1.0195 mL 2.0389 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.75%

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Product Name:
IDH-305
Cat. No.:
HY-104036
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