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533717 Sigma-AldrichGLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem

Cell-permeable, orally available, potent, selective & non-competitive GLS1 inhibitor. Reduces glutamine consumption & glutamate secretion, and induces apoptosis.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: N-(6-(4-(5-((2-Pyridin-2-ylacetyl)amino)-1,3,4-thiadiazol-2-yl)butyl)pyridazin-3-yl)-2-(3-(trifluoromethoxy)phenyl)acetamide, KGA Inhibitor III, 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide, GAC Inhibitor III, Kidney-Type Glutaminase Inhibitor III

Primary Target: GLS1

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1439399-58-2	C₂₆H₂₄F₃N₇O₃S

价格及供货情况

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Description
Overview	A cell-permeable, orally available thiadiazolyl-butyl-pyridazinyl compound that acts as a potent, selective, time-dependent, and slowly-reversible (t_1/2 = 45 min at 25 °C) inhibitor of glutaminase (IC₅₀ = 45, 23 and 28 nM for rec hu-GAC, KGA and GAC, respectively). The inhibition appears to be non-competitive and allosteric. Exhibits anti-proliferative effects in HCC1806 and MDA-MB-231 triple-negative breast cancer cell lines (IC₅₀ = 49 and 26 nM, respectively), but does not affect the viability of ER+/HER2-T47D cell line. Shown to reduce glutamine consumption (IC₅₀ = 17 nM) and glutamate production (IC₅₀ = 15 nM) rates in HCC1806 cells. Inhibits the growth of HCC1806 xenografts in mice (~200 mg/kg, p.o., b.i.d) and of JIMT-1 xenografts (200 mg/kg p.o., b.i.d), either alone or in combination with paclitaxel (10 mg/kg , 5 doses alternate days). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number	533717
Brand Family	Calbiochem®
Synonyms	N-(6-(4-(5-((2-Pyridin-2-ylacetyl)amino)-1,3,4-thiadiazol-2-yl)butyl)pyridazin-3-yl)-2-(3-(trifluoromethoxy)phenyl)acetamide, KGA Inhibitor III, 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide, GAC Inhibitor III, Kidney-Type Glutaminase Inhibitor III
Description	GLS1 Inhibitor III, CB-839

References
References	Gross, M.I., et al. 2014. Mol. Cancer Ther. 13, 890.

Product Information
CAS number	1439399-58-2
Form	Yellow to brown solid
Hill Formula	C₂₆H₂₄F₃N₇O₃S
Chemical formula	C₂₆H₂₄F₃N₇O₃S
Reversible	Y
Quality Level	MQ100

Applications

Biological Information
Primary Target	GLS1
Primary Target IC<sub>50</sub>	23 nM & 28 nM, respectively, using murine kidney and brain homogenates
Purity	≥97% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.33717.0001	04055977286656

Documentation

GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem 分析证书

标题	批号
533717	输入批号

参考

参考信息概述
Gross, M.I., et al. 2014. Mol. Cancer Ther. 13, 890.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	26-August-2024 JSW
Synonyms	N-(6-(4-(5-((2-Pyridin-2-ylacetyl)amino)-1,3,4-thiadiazol-2-yl)butyl)pyridazin-3-yl)-2-(3-(trifluoromethoxy)phenyl)acetamide, KGA Inhibitor III, 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide, GAC Inhibitor III, Kidney-Type Glutaminase Inhibitor III
Description	A cell-permeable thiadiazolyl-butyl-pyridazinyl compound that selectively inhibits GLS1 (IC₅₀ = 23 nM & 28 nM, respectively, using murine kidney and brain homogenates), but not GLS2/LGA (up to 5 µM using murine liver homogenates), glutaminase activity in a non-competitive manner, being more potent than the uncompetitive GLS1 inhibitor BPTES, but with much slower inhibition kinetics (IC₅₀/preincubation time ~300 nM/1 min & & 50 nM/1 h for CB-839; 630 nM/1 min & 700 nM/1 h for BPTES; 2 nM rhGAC aa 126-598) & reversibility (Activity recovery t_1/2 after free drug removal = 45 min/CB-839 & <3 min/BPTES). CB-839 also displays higher antiproliferation potency than BPTES against triple negative breast cancer (TNBC) cultures (GI₅₀ against MDA-MB-231 in 72 h = 19 nM vs. 2.4 µM with BPTES; GI₅₀ against HCC1806 in 72 h = 55 nM vs. 2.0 µM with BPTES), while neither drug is effective against GLS1-independent growth of estrogen receptor-positive T47D even at 1 µM concentration. Despite a fast clearance in mice (Plasma t_1/2 <2 h post 50 mg/kg p.o.), good drug exposure is reported in tumor and major organs (>1 nmol/g) 4 h post single 200 mg/10 mL/kg oral dosage among HCC1806 xenograft mice (Drug conc. = 2.1 µM in Plasma & 1.5 nmol/g in 500 mm³ tumor) except brain (~0.2 nmol/g) with most pronounced Glutamine buildup observed in tumor (5-fold) when compared to normal tissues (1- to 2.28-fold of of no treatment controls). Twice daily oral administration (200 mg/kg/12 h) is efficacious in suppressing the expansion of established tumor derived from HIMT-1 (by 54% in 35 d) and patient TNBC (by 59% in 28 d) and complete suppression of JIMT-1 tumor is seen when combined with 5 daily doses of Paclitaxel (10 mg/kg i.v.; Cat. Nos. 580555 & 580556) in the first 5 d of the treatment period.
Form	Yellow to brown solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1439399-58-2
Chemical formula	C₂₆H₂₄F₃N₇O₃S
Purity	≥97% by HPLC
Solubility	DMSO (25 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Gross, M.I., et al. 2014. Mol. Cancer Ther. 13, 890.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Proteases Inhibitors

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