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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  protein tyrosine kinase >  3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide

3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide

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3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide Basic information

Product Name:
3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide
Synonyms:
  • 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide
  • MK-8033
  • 1-(3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl)-N-(pyridin-2-ylmethyl)methanesulfonamide
  • 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinyLMethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridin
  • CS-2738
  • MK 8033;MK8033
  • CS-1167
  • 100853
CAS:
1001917-37-8
MF:
C25H21N5O3S
MW:
471.53
Mol File:
1001917-37-8.mol
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3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide Chemical Properties

Boiling point:
761.0±70.0 °C(Predicted)
Density 
1.39
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
pka
8.93±0.40(Predicted)
form 
Powder
color 
Light yellow to yellow
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3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide Usage And Synthesis

Uses

MK 8033 is a novel and specific dual ATP competitive c-Met/Ron inhibitor and is used in the treatment of cancer.

in vivo

MK-8033 (Compound 11r, oral administration, 3-100 mg/kg, twice daily for 21 days) inhibits tumor growth in GTL-16 c-Met amplified gastric tumor xenografts[1].
MK-8033 exhibits moderate clearance (t1/2: 0.8 h for rats, 3.1 h for dog) and favorable bioavailability (35% for rats, 33% for dog)[1].

Animal Model:Human GTL-16 c-Met amplified gastric tumor xenografts[1]
Dosage:3, 10, 30, and 100 mg/kg
Administration:Oral administration, twice daily for 21 days
Result:Resulted in 22, 18, 57, and 86% tumor growth inhibition at 3, 10, 30, and 100 mg/kg, respectively.
Inhibited c-Met (Y1349) phosphorylation.

IC 50

Ron: 7 nM (IC50)

3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamideSupplier

Shanghai Boyle Chemical Co., Ltd.
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