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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 | Availability | Quantity |
---|---|---|---|
1 mg | 49 € | In Stock | |
5 mg | 121 € | In Stock | |
10 mg | 169 € | In Stock | |
25 mg | 350 € | In Stock | |
50 mg | 530 € | In Stock | |
1 mL x 10 mM (in DMSO) | 132 € | 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 (R132H):27 nM, IDH1 (R132C):28 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (203.90 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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