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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $52 | In Stock | In Stock | |
| 5 mg | $128 | In Stock | In Stock | |
| 10 mg | $178 | In Stock | In Stock | |
| 25 mg | $369 | In Stock | In Stock | |
| 50 mg | $558 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $139 | In Stock | In Stock |
| 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 (WT):6.14 μM, IDH1 (R132C):28 nM, IDH1 (R132H):27 nM |
| 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]. |
| Molecular Weight | 490.45 |
| Formula | C23H22F4N6O2 |
| Cas No. | 1628805-46-8 |
| Smiles | C[C@H](F)[C@H]1COC(=O)N1c1ccnc(N[C@@H](C)c2cc(C)c(cn2)-c2ccnc(c2)C(F)(F)F)n1 |
| Relative Density. | 1.370 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (203.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.16 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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