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Crelosidenib
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Catalog No. T39716Cas No. 2230263-60-0
Alias Mutant IDH1-IN-6, LY3410738, LY 3410738
Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.
Crelosidenib
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Purity: 98.54%
Catalog No. T39716Alias Mutant IDH1-IN-6, LY3410738, LY 3410738Cas No. 2230263-60-0
Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $397 | - | In Stock | |
| 5 mg | $970 | - | In Stock | |
| 10 mg | $1,290 | - | In Stock | |
| 25 mg | $1,950 | - | In Stock | |
| 50 mg | $2,620 | - | In Stock | |
| 100 mg | $3,530 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.54%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme. |
| Targets&IC50 | HT1080 cells:1.28 nM |
| In vitro | Crelosidenib (Example 2) suppresses 2-hydroxyglutarate production in HT1080 cells with an IC₅₀ of 1.28 nM, demonstrating effective inhibition of mutant IDH1 R132C activity in a cellular context. The level of α-ketoglutarate (aKG), a product of wild-type IDH1, remains unchanged, confirming the compound’s selectivity for the mutant enzyme over the wild-type form[1]. |
| In vivo | Treatment with Crelosidenib (Example 2) via oral gavage at doses ranging from 0 to 32 mg/kg, administered twice daily for 3 days, resulted in a dose-dependent reduction of 2-hydroxyglutarate levels in xenograft mice bearing IDH1 mutations[1]. |
| Synonyms | Mutant IDH1-IN-6, LY3410738, LY 3410738 |
| Molecular Weight | 504.62 |
| Formula | C28H36N6O3 |
| Cas No. | 2230263-60-0 |
| Smiles | [C@H](CC1CC1)(C2=CC=C([C@@H](NC=3N=C4C(=CN3)COC(=O)N4CC)C)C=C2)N5CCN(C(C=C)=O)CC5 |
| Relative Density. | 1.251 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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