GSK-864 free base · Synonyms: GSK 864 · GSK864

GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and…

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

Target Isocitrate Dehydrogenase (IDH)

Research area Cancer

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Data Sheet SDS COA

GSK-864 structure

CAS No.: 1816331-66-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 750.00	BP-02224-50mg	In stock	Get quote
100 mg	USD 985.00	BP-02224-100mg	In stock	Get quote
250 mg	USD 1,385.00	BP-02224-250mg	In stock	Get quote
500 mg	USD 2,385.00	BP-02224-500mg	In stock	Get quote
1 g	USD 3,685.00	BP-02224-1g	In stock	Get quote
5 g	Inquire	BP-02224-5g	In stock	Inquire

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Description

GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.

Biological activity

In Vitro GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC50 of 320 nM by LCMS/MS analysis In Vivo Following intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45+ CD38+ cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864

Identifiers

SMILES: CC1=CC(=CC(=C1OC)C)NC(=O)C2=NN(C3=C2CN(C[C@]3(C)C(=O)N)C(=O)C4=CC=CN4)CC5=CC=C(C=C5)F
InChIKey: DUCNNEYLFOQFSW-PMERELPUSA-N

Specifications

MW (average): 558.6033
Formula: C₃₀H₃₁FN₆O₄
CAS No.: 1816331-66-4
Physical state: Solid
Color: Light brown to brown
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

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Okoye-Okafor UC, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86.

Same target

Search Isocitrate Dehydrogenase (IDH)

Same research area

Search Cancer