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Purity: ≥98%
Olutasidenib (FT-2102) is a novel, highly potent and selective small molecue inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1) with the potential to be used in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Isocitrate dehydrogenase 1 mutations (IDH1m) occur in 7-14% of AML patients (pts) and 3% of MDS pts. FT-2102 has shown favorable safety, PK/PD, and clinical activity in IDH1m AML/MDS with a single agent complete response rate (CR/CRi) of 38% and a complete response rate of 27% in combination with AZA. Current data support the continued evaluation of 150 mg BID in the expansion and Phase 2 stages of the study.
| ln Vitro |
Numerous IDH1-R132 mutants (R132H, R132C, R132G, and R132L) can effectively be inhibited from producing 2-HG by olutasidenib (FT-2102), suggesting that Olutasidenib (FT-2102) is effective against the majority of tumors expressing IDH1-R132 mutants. IDH1 isoforms are the only ones that olintasidenib (FT-2102) significantly inhibits, with no discernible effect on wild-type IDH1 (> 20 µM) or IDH2 mutants (R172K and R140Q, both > 20 µM) [2].
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| ln Vivo |
Three oral doses of olinusidenib (FT-2102; 25 mg/kg, 50 mg/kg, and 12 hours apart) showed strong antitumor activity in xenografted female BALB/c nude mice with the HCT116-IDH1-R132H/+ mutation [2].
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| Animal Protocol |
Animal/Disease Models: HCT116-IDH1-R132H/+ xenograft-bearing female BALB/c nude mice [2].
Doses: 12.5, 25 and 50 mg/kg. Doses: Orally administered 3 times (12.5, 25 and 50 mg/kg) every 12 hrs (hrs (hours)). Experimental Results: Demonstrated time- and dose-dependent inhibition of 2-HG levels in tumors. At the highest dose tested in these studies (50 mg/kg), FT-2102 treatment inhibited 2-HG levels in tumors by >90% within 24 hrs (hrs (hours)) of the last dose in HCT116-IDH1-R132H/+ Xenograft model. |
| References |
[1]. JM Watts, et al. A phase 1 dose escalation study of the IDH1m inhibitor, FT-2102, in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
[2]. Justin A. Caravella, et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J Med Chem. 2020. |
| Molecular Formula |
C18H15CLN4O2
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|---|---|
| Molecular Weight |
354.79030251503
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| CAS # |
1887014-12-1
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| SMILES |
N#CC1=CC=C(N[C@H](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)C(N1C)=O
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| InChi Key |
NEQYWYXGTJDAKR-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1
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| Chemical Name |
5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
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| Synonyms |
FT-2102; FT 2102; FT2102
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~352.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8186 mL | 14.0928 mL | 28.1857 mL | |
| 5 mM | 0.5637 mL | 2.8186 mL | 5.6371 mL | |
| 10 mM | 0.2819 mL | 1.4093 mL | 2.8186 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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