Basic information Safety Supplier Related

Takinib

Basic information Safety Supplier Related

Takinib Basic information

Product Name:
Takinib
Synonyms:
  • Takinib
  • 1-N-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide
  • N-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide
  • 3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide
  • N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide
  • EDHS-206
  • 1,3-Benzenedicarboxamide, N1-(1-propyl-1H-benzimidazol-2-yl)-
  • Takinib >=98% (HPLC)
CAS:
1111556-37-6
MF:
C18H18N4O2
MW:
322.36
Mol File:
1111556-37-6.mol
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Takinib Chemical Properties

Density 
1.30±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:30.0(Max Conc. mg/mL);93.06(Max Conc. mM)
form 
A solid
pka
12.13±0.43(Predicted)
color 
White to off-white
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Takinib Usage And Synthesis

Uses

Takinib has been used as an inhibitor of transforming 28 growth factor - β-activated kinase -1 (TAK-1) in human leukemia monocytic THP-1 cells. It may be used as a TAK1 inhibitor in Jurk at cells.

Biological Activity

Takinib is a selective inhibitor of TAK1/MAP3K7 kinase, which is a member of the MAP3K family and a key regulator of cell death. It binds in the TAk1 ATPbinding pocket with an IC50 value of 9.5 nM. Takinib selectively induced apoptosis following TNF-α stimulation in rheumatoid arthritis and breast cancer.

in vivo

Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis[4].
Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].

Animal Model:Male DBA/1 mice (CIA arthritis model)[4]
Dosage:50 mg/kg
Administration:Intraperitoneally; daily from days 18-36
Result:Showed a reduction in clinical arthritic score compared to vehicle control.
Animal Model:Female NSG mice (8 weeks old)[5]
Dosage:50 mg/kg
Administration:Oral gavage; daily until 17 days
Result:Slowed tumor growth and reduced tumor size/weight.

IC 50

TAK1: 9.5 nM (IC50); IRAK4: 120 nM (IC50); IRAK1: 390 nM (IC50); GCK: 430 nM (IC50); CLK2: 430 nM (IC50); MINK1: 1.9 μM (IC50)

storage

Store at -20°C

TakinibSupplier

Nanjing Dulai Biotechnology Co., Ltd.
Tel
025-846993838003-8003 18013301590
Email
njduly@126.com
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Email
info@adooq.cn
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Email
sales@shjiyipharmatech.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Email
sales@zehanbiopharma.com
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