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IDH-305

Catalog No. T15550Cas No. 1628805-46-8

IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.

IDH-305

IDH-305

Purity: 99.13%
Catalog No. T15550Cas No. 1628805-46-8
IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$52In Stock
5 mg$128In Stock
10 mg$178In Stock
25 mg$369In Stock
50 mg$558In Stock
1 mL x 10 mM (in DMSO)$139In Stock
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Purity:99.13%
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Product Introduction

Bioactivity
Description
IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.
Targets&IC50
IDH1 (R132C):28 nM, IDH1 (R132H):27 nM, IDH1 (WT):6.14 μM
In vitro
IDH-305 suppresses HCT116-IDH1R132H /- cells (IC50 of 24 nM)[1].
In vivo
P.o. administration of 30-300 mg/kg IDH-305 twice daily for 21 days suppresses 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model [1].
Chemical Properties
Molecular Weight490.45
FormulaC23H22F4N6O2
Cas No.1628805-46-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (203.90 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0389 mL10.1947 mL20.3894 mL101.9472 mL
5 mM0.4078 mL2.0389 mL4.0779 mL20.3894 mL
10 mM0.2039 mL1.0195 mL2.0389 mL10.1947 mL
20 mM0.1019 mL0.5097 mL1.0195 mL5.0974 mL
50 mM0.0408 mL0.2039 mL0.4078 mL2.0389 mL
100 mM0.0204 mL0.1019 mL0.2039 mL1.0195 mL

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