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G007-LK

Product Name
G007-LK
CAS No.
1380672-07-0
Chemical Name
G007-LK
Synonyms
G007-LK;CS-1659;G007 LK;G007LK;G007-LK;G007 LK;G007LK;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile;Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
CBNumber
CB32707548
Molecular Formula
C25H16ClN7O3S
Formula Weight
529.96
MOL File
1380672-07-0.mol
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G007-LK Property

Boiling point:
817.3±75.0 °C(Predicted)
Density 
1.47±0.1 g/cm3(Predicted)
storage temp. 
+2C to +8C
solubility 
≥26.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form 
White powder
pka
-1.68±0.10(Predicted)
color 
Off-white to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.04907
Product name
Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
Purity
Tankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively).
Packaging
10MG
Price
$280
Updated
2024/03/01
Cayman Chemical
Product number
22934
Product name
G007-LK
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
22934
Product name
G007-LK
Purity
≥98%
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
22934
Product name
G007-LK
Purity
≥98%
Packaging
10mg
Price
$243
Updated
2024/03/01
Cayman Chemical
Product number
22934
Product name
G007-LK
Purity
≥98%
Packaging
25mg
Price
$533
Updated
2024/03/01
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G007-LK Chemical Properties,Usage,Production

General Description

A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biological Activity

g007-lk is a potent and specific inhibitor of tankyrase 1/2 with ic50 values of 46 and 25 nm [1].the telomeric repeat factor 1 (trf1)-interacting ankyrin-related adp-ribose polymerase 1 (tankyrase 1,tnks1) and tankyrase 2 (tnks2) belong to the subgroup of poly(adp-ribosyl)ating polymerases and regulate the assembly and disassembly of large polymerized structures [1].g007-lk is a potent and specific tankyrase 1/2 inhibitor. g007-lk reduced auto-poly-(adp ribosy)lation of tnks1 and tnks2 with ic50 values of 46 nm and 25 nm, respectively. in wnt3a-induced hek 293 cells, g007-lk inhibited st-luc with ic50 value of 0.05 μm [1]. in sw480 colorectal cancer cell line transfected with gfp-tnks1, g007-lk induces highly dynamic and mobile degradasomes containing phosphorylated beta-catenin, beta-trcp and ubiquitin [2]. in the apc-mutant cell lines, g007-lk reduces cytosolic and nuclear β-catenin protein levels [3].in mice bearing colo-320dm cell xenografts, g007-lk (20 mg/kg twice daily or 40 mg/kg daily) concentration-dependently inhibited tumor growth by 61% and 48%, respectively. also, g007-lk reduced the levels of tnks1/2 and β-catenin, and stabilized axin1/2 [3].

Biochem/physiol Actions

Cell permeable: yes

References

[1]. voronkov a, holsworth dd, waaler j, et al. structural basis and sar for g007-lk, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. j med chem, 2013, 56(7): 3012-3023.
[2]. thorvaldsen te, pedersen nm, wenzel em, et al. structure, dynamics and functionality of tankyrase inhibitor-induced degradasomes. mol cancer res, 2015, pii: molcanres.0125.2015.
[3]. lau t, chan e, callow m, et al. a novel tankyrase small-molecule inhibitor suppresses apc mutation-driven colorectal tumor growth. cancer res, 2013, 73(10): 3132-3144.

G007-LK Preparation Products And Raw materials

Raw materials

Preparation Products

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G007-LK Suppliers

China 72 India 1 United Kingdom 1 United States 10 Global 84
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4727
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Hangzhou J&H Chemical Co., Ltd.
Tel
0571-+86-571-87396432
Fax
0571-87396431
Email
sales@jhechem.com
Country
China
ProdList
11578
Advantage
59
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4565
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
1004
Advantage
55
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View Lastest Price from G007-LK manufacturers

Career Henan Chemical Co
Product
(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile 1380672-07-0
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2020-01-01

1380672-07-0, G007-LKRelated Search:


  • G007-LK
  • (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
  • 4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
  • Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
  • G007-LK;G007 LK;G007LK
  • CS-1659
  • Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
  • G007 LK;G007LK
  • G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK
  • 1380672-07-0
  • C25H16ClN7O3S