Olutasidenib (FT-2102)

Olutasidenib (FT-2102) 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.TargetsIDH1 (R132H) (Cell-free assay); IDH1 (R132C) (Cell-free assay) 21.1 nM; 114 nMIn vitroProfiling 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 vivoIn 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..Cell Research(from reference)Cell lines：HCT116-IDH1-R132H/+, HCT116-IDH1-R132C/+, HT1080, U87MG cells Incubation Time：24 h

Dehydrogenase Inhibitors

Specifications & Purity: Olutasidenib (FT-2102) 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.TargetsIDH1 (R132H) (Cell-free assay); IDH1 (R132C) (Cell-free assay) 21.1 nM; 114 nMIn vitroProfiling 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 vivoIn 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..Cell Research(from reference)Cell lines：HCT116-IDH1-R132H/+, HCT116-IDH1-R132C/+, HT1080, U87MG cells Incubation Time：24 h

Grade: Moligand™

Molecular Formula: C18H15ClN4O2 

Molecular Weight: 354.79

EC Number: 112-748-6

PubChem CID: 118955396

Isomeric SMILES: C[C@@H](C1=CC2=C(C=CC(=C2)Cl)NC1=O)NC3=CC=C(N(C3=O)C)C#N

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads

More Information: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/O414289-SCI_34ea699b5fe26eb29679c64f62872757.pdf

UPC:

51112010

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

O414289-1mg

Country of Origin:

China

CAS:

1887014-12-1

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90