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Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $56 | In Stock | |
5 mg | $172 | In Stock | |
10 mg | $278 | In Stock | |
25 mg | $513 | In Stock | |
50 mg | $747 | In Stock | |
100 mg | $1,050 | In Stock | |
200 mg | $1,390 | In Stock | |
1 mL x 10 mM (in DMSO) | $188 | In Stock |
Description | Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively). |
Targets&IC50 | IDH1 (R132C):114 nM (IC50), IDH1 (R132H):21.2 nM (IC50) |
In vitro | Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (> 20 μM) and IDH2 mutants (R172K and R140Q: both > 20 μM). Olutasidenib effectively suppresses 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), displaying Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors [2]. |
In vivo | In HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice, Olutasidenib (three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) shows effective anti-tumor activity [2]. |
Alias | FT-2102 |
Molecular Weight | 354.79 |
Formula | C18H15ClN4O2 |
Cas No. | 1887014-12-1 |
Smiles | C[C@H](Nc1ccc(C#N)n(C)c1=O)c1cc2cc(Cl)ccc2[nH]c1=O |
Relative Density. | 1.42 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 122 mg/mL (343.87 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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