Olutasidenib free base · Synonyms: FT-2102

Olutasidenib is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1.

For research use only. Not for human or veterinary use.

Target Isocitrate Dehydrogenase (IDH)

Research area Inflammation/Immunology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Olutasidenib structure

CAS No.: 1887014-12-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 560.00	BP-01947-250mg	In stock	Get quote
500 mg	USD 880.00	BP-01947-500mg	In stock	Get quote
1 g	USD 1,480.00	BP-01947-1g	In stock	Get quote
2 g	Inquire	BP-01947-2g	Inquire	Inquire
5 g	Inquire	BP-01947-5g	Inquire	Inquire

Need another size or custom synthesis? Request a quote.

Description

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.

Biological activity

In Vitro Olutasidenib (FT-2102) potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib (FT-2102) 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)[2]. 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].

Identifiers

SMILES: N#CC1=CC=C(N[C@H](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)C(N1C)=O
InChIKey: NEQYWYXGTJDAKR-JTQLQIEISA-N

Specifications

MW (average): 354.7900
Formula: C₁₈H₁₅ClN₄O₂
CAS No.: 1887014-12-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

Same target

Search Isocitrate Dehydrogenase (IDH)

BP-02224 GSK-864 free base · >98%

Same research area

Search Inflammation/Immunology