Olutasidenib
- Product Name
- Olutasidenib
- CAS No.
- 1887014-12-1
- Chemical Name
- Olutasidenib
- Synonyms
- FT-2102;OLUTASIDENIB;Olutasidenib (FT-2102);Olutasidenib, 10 mM in DMSO;Olutasidenib (FT-2102) ,S8949;Olutasidenib (Synonyms: FT-2102);mutant,FT2102,inhibit,Isocitrate Dehydrogenase (IDH),Olutasidenib,2-HG,FT 2102,Inhibitor;(S)-5-[[1-(6-Chloro-2-oxo-1,2-dihydro-3-quinolyl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile;(S)-5-((1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile;5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
- CBNumber
- CB04845034
- Molecular Formula
- C18H15ClN4O2
- Formula Weight
- 354.79
- MOL File
- 1887014-12-1.mol
Olutasidenib Property
- Boiling point:
- 603.3±55.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: soluble
- form
- A crystalline solid
- pka
- 10.44±0.70(Predicted)
- color
- Light yellow to yellow
- InChI
- 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
- InChIKey
- NEQYWYXGTJDAKR-JTQLQIEISA-N
- SMILES
- C1(C#N)N(C)C(=O)C(N[C@H](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)=CC=1
N-Bromosuccinimide Price
- Product number
- CS-0080183
- Product name
- Olutasidenib
- Purity
- 98.35%
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0080183
- Product name
- Olutasidenib
- Purity
- 98.35%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0080183
- Product name
- Olutasidenib
- Purity
- 98.35%
- Packaging
- 25mg
- Price
- $700
- Updated
- 2021/12/16
- Product number
- CS-0080183
- Product name
- Olutasidenib
- Purity
- 98.35%
- Packaging
- 50mg
- Price
- $1100
- Updated
- 2021/12/16
- Product number
- orb611286
- Product name
- Olutasidenib (FT-2102)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1431.4
- Updated
- 2021/12/16
Olutasidenib Chemical Properties,Usage,Production
Uses
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1][2].
Mechanism of action
Olutasidenib specifically inhibits the mutant IDH1 enzyme, which reduces the accumulation of abnormal metabolites and promotes normal differentiation and maturation of cells. This targeted treatment approach aims to reduce tumor burden and improve patient outcomes.
in vivo
Olutasidenib (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2].
| Animal Model: | HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2]. |
| Dosage: | 12.5, 25, and 50 mg/kg. |
| Administration: | Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals. |
| Result: | Showed a time and dose-dependent inhibition of 2-HG levels in in tumor. At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model. |
IC 50
IDH1
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.
Olutasidenib Preparation Products And Raw materials
Raw materials
Preparation Products
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