CasNo.1439399-58-2,Telaglenastat (CB-839),(1439399-58-2) Suppliers

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Purity: >97%

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Telaglenastat CB-839 1439399-58-2

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Biological Activity

Description

Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.

Targets

Glutaminase [1]
(Cell-free assay)

24 nM

In vitro

CB-839 exhibits time-dependent and slowly reversible kinetics. IC50 values for glutaminase inhibition by CB-839 following preincubation with rHu-GAC for-1 hour are < 50 nmol/L, at least 13-fold lower than with BPTES. CB-839 has antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, while no antiproliferative activity is observed in an estrogen receptor–positive cell line, T47D.[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
MDA-MB-231 cells	Cytotoxicity assay		6 days	Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry, IC50=0.033 μM	26988803
TNBC cell lines	Growth inhibiton assay	1 μM	4 days	CB-839 treatment induced cell loss or decreased cell proliferation by more than 50% in six cell lines (HCC1806, HCC1143, HCC38, MDA-MB-436, MDA-MB-231 and Hs578T); the other six cell lines (HCC1937, HCC70, BT549, MDA-MB-157, MDA-MB-453 and MDA-MB468) were either not affected or had their cell proliferation affected by less than 50% and were called resistant.	31040181
MM.1S BzR cells	Function assay	5 μM	16 hours	treatment with CB-839 significantly repressed oxygen consumption rate in proteasome-inhibitor resistant cells.	28415782

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Assay

Methods	Test Index	PMID
Western blot	collagen I/collagen III;	29019707
Growth inhibition assay	Cell growth;	28967864

In vivo

In the mouse TNBC model, single agent CB-839 (200 mg/kg, p.o.) suppresses tumor growth by 61% relative to vehicle control. In the mouse JIMT-1 xenograft model, CB-839 alone (200 mg/kg, p.o.) results in 54% tumor growth inhibition (TGI) relative to vehicle control, combination of CB-839 (200 mg/kg, p.o.) with paclitaxel (10 mg/kg, p.o.) largely suppresses the regrowth of the tumors resulting in a TGI relative to vehicle control of 100%.[1]