Product Name :
Olutasidenib (FT-2102)
Description:
Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.
CAS:
1887014-12-1
Molecular Weight:
354.79
Formula:
C18H15ClN4O2
Chemical Name:
5-[1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
Smiles :
CC(NC1=CC=C(C#N)N(C)C1=O)C1=CC2C=C(Cl)C=CC=2NC1=O
InChiKey:
NEQYWYXGTJDAKR-UHFFFAOYSA-N
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.GLP-1(7-37) manufacturer
Additional information:
Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.|Product information|CAS Number: 1887014-12-1|Molecular Weight: 354.Dabigatran etexilate web 79|Formula: C18H15ClN4O2|Synonym:|FT-2102|Chemical Name: 5-[1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile|Smiles: CC(NC1=CC=C(C#N)N(C)C1=O)C1=CC2C=C(Cl)C=CC=2NC1=O|InChiKey: NEQYWYXGTJDAKR-UHFFFAOYSA-N|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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 122 mg/mL (343.87mM), Need ultrasonic|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.PMID:32762354 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Profiling in various mIDH1 over-expressing U87 cells and HCT116 cells reveals that olutasidenib potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting olutasidenib could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 and IDH2 mutants..|In Vivo:|In IDH1-R132H/ xenograft models, the free concentration of Olutasidenib is comparable in plasma and xenograft tumors, and exposures are dose-dependent. In comparison to the vehicle treated group, Olutasidenib shows a time and dose-dependent inhibition of 2-HG levels in tumor. Calculations based upon the percentage of suppression of 2-HG concentration in tumor versus the free drug concentration in tumor give in vivo IC50 values of 26 nM and 36 nM in the HCT116-IDH1-R132H or HCT116-IDH1-R132C models, respectively. Olutasidenib has good cell permeability and low efflux ratio in the male CD-1 mouse, which indicate a low probability of p-glycoprotein driven efflux..|References:|Justin A. Caravella, et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J Med Chem. 2020.Products are for research use only. Not for human use.|
