Description In vitro In vivo
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CB-839

Description In vitro In vivo
Product Name
CB-839
CAS No.
1439399-58-2
Chemical Name
CB-839
Synonyms
CB-839;CPD1593;CS-1813;Telaglenastat;CB-839,TELAGLENASTAT;CB839 ;CB 839 ;CB-839;Telaglenastat (CB-839);GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem;N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide;2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-
CBNumber
CB92718863
Molecular Formula
C26H24F3N7O3S
Formula Weight
571.57
MOL File
1439399-58-2.mol
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CB-839 Property

Melting point:
186- 189° C
Density 
1.430±0.06 g/cm3(Predicted)
storage temp. 
+2C to +8C
solubility 
Soluble in DMSO.
form 
Yellow solid
pka
8.25±0.50(Predicted)
color 
Pale yellow
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.33717
Product name
GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem
Packaging
10mg
Price
$258
Updated
2024/03/01
Cayman Chemical
Product number
22038
Product name
CB-839
Purity
≥98%
Packaging
5mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
22038
Product name
CB-839
Purity
≥98%
Packaging
50mg
Price
$302
Updated
2024/03/01
Cayman Chemical
Product number
22038
Product name
CB-839
Purity
≥98%
Packaging
1mg
Price
$30
Updated
2021/12/16
Cayman Chemical
Product number
22038
Product name
CB-839
Purity
≥98%
Packaging
10mg
Price
$95
Updated
2024/03/01
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CB-839 Chemical Properties,Usage,Production

Description

CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

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.

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%.

Description

CB-839 (14393999-58-2)?is a potent (IC50?= 24 nM), selective and orally bioavailable inhibitor of glutaminase (KGA and GAC).1?CB-839 displayed an antiproliferative effect in the triple-negative breast cancer cell line, HCC-1806, but no activity in the estrogen receptor-positive cell line T47D.? CB-839 was able to cause proliferation arrest and apoptosis in acute myeloid leukemia cells without causing cytotoxicity against normal human CD34(+) progenitors.2? Aspartate-glutamate carrier 1 (AGC1) inhibition can synergize with CB-839 to limit tumor growth.3

Uses

CB-839 performs an antileukemic activity. It Inhibits GLS1 genes and reduces oxidative phosphorylation leading to leukamic cell proliferation arrest and apoptosis.

storage

Store at -20°C

References

1) Gross?et al. (2014),?Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer; Mol. Cancer Ther.,13?890 2) Jacque?et al. (2015),?Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition; Blood,?126?1346 3) Alkan?et al.?(2018)?Cytosolic Aspartate Availability Determines Cell Survival When Glutamine is Limiting; Cell Metabolism?28?1

CB-839 Preparation Products And Raw materials

Raw materials

Preparation Products

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CB-839 Suppliers

AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
Alfa Chemistry
Tel
Fax
1-516-927-0118
Email
Info@alfa-chemistry.com
Country
United States
ProdList
24072
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38631
Advantage
58
ApexBio Technology
Tel
--
Fax
--
Email
sales@apexbt.com
Country
United States
ProdList
6251
Advantage
58
Focus Biomolecules
Tel
--
Fax
--
Email
sales@focusbiomolecules.com
Country
United States
ProdList
1284
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58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
United States Biological
Tel
--
Fax
--
Email
chemicals@usbio.net
Country
United States
ProdList
6214
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80
Riedel-de Haen AG
Tel
--
Fax
--
Country
United States
ProdList
6773
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87
Selleck Chemicals LLC
Tel
--
Fax
--
Email
info@selleckchem.com
Country
United States
ProdList
824
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60
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View Lastest Price from CB-839 manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
CB-839 1439399-58-2
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1Ton
Release date
2022-10-13

1439399-58-2, CB-839Related Search:


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  • 2-(pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide
  • CPD1593
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  • CB839 ;CB 839 ;CB-839
  • GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem
  • CB-839,TELAGLENASTAT
  • Telaglenastat
  • CS-1813
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  • Telaglenastat (CB-839)
  • Glutaminase,antiproliferative,HCC-1806,TNBC,Telaglenastat,breast,Inhibitor,Autophagy,splice,cell,PDAC,variants,selective,cancer,triple-negative,inhibit
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