CB-839 free base · Synonyms: Telaglenastat

Telaglenastat is a first-in-class, reversible and orally bioavailable glutaminase 1 inhibitor.

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

Target Autophagy Glutaminase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CB-839 structure

CAS No.: 1439399-58-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 480.00	BP-01890-1g	In stock	Get quote
2 g	USD 780.00	BP-01890-2g	In stock	Get quote
5 g	Inquire	BP-01890-5g	Inquire	Inquire
10 g	Inquire	BP-01890-10g	Inquire	Inquire

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Description

Telaglenastat (CB-839) is a first-in-class, reversible and orally bioavailable glutaminase 1 (GLS1) inhibitor. Telaglenastat (CB-839) selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2.

Biological activity

In Vitro Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively. Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells. In Vivo Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC.

Identifiers

SMILES: FC(F)(F)OC1=CC(CC(=O)NC2=NN=C(CCCCC3=NN=C(NC(=O)CC4=NC=CC=C4)S3)C=C2)=CC=C1
InChIKey: PRAAPINBUWJLGA-UHFFFAOYSA-N

Specifications

MW (average): 571.5740
Formula: C₂₆H₂₄F₃N₇O₃S
CAS No.: 1439399-58-2
Physical state: Solid
Color: Off-white 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

In vitro: DMSO : 35 mg/mL

Documents

References

[1]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.

[2]. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965.

[3]. Zhou WJ, et al. Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun Signal. 2019 Aug 20;17(1):99.

Same target

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Same research area

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