ChemicalBook > CAS DataBase List > MK-8033 (hydrochloride)

MK-8033 (hydrochloride)

Product Name
MK-8033 (hydrochloride)
CAS No.
1283000-43-0
Chemical Name
MK-8033 (hydrochloride)
Synonyms
MK-8033 HCl;MK-8033 (hydrochloride);MK8033 HYDROCHLORIDE;MK 8033 HYDROCHLORIDE;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 hydrochloride;3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide hydrochloride (1:1)
CBNumber
CB52677049
Molecular Formula
C25H22ClN5O3S
Formula Weight
507.99
MOL File
1283000-43-0.mol
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MK-8033 (hydrochloride) Property

storage temp. 
under inert gas (nitrogen or Argon) at 2-8°C
solubility 
DMSO : < 1 mg/mL (insoluble or slightly soluble)
form 
Powder
color 
Light yellow to yellow
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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

ChemScene
Product number
CS-1849
Product name
MK-8033hydrochloride
Purity
99.70%
Packaging
5mg
Price
$456
Updated
2021/12/16
ChemScene
Product number
CS-1849
Product name
MK-8033hydrochloride
Purity
99.70%
Packaging
10mg
Price
$696
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611564
Product name
MK-8033 hydrochloride
Packaging
100mg
Price
$1654.1
Updated
2021/12/16
ChemScene
Product number
CS-1849
Product name
MK-8033hydrochloride
Purity
99.70%
Packaging
50mg
Price
$1656
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611564
Product name
MK-8033 hydrochloride
Packaging
250mg
Price
$3282.7
Updated
2021/12/16
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MK-8033 (hydrochloride) Chemical Properties,Usage,Production

Uses

MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs)[1][2].

in vivo

MK-8033 hydrochloride (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 hydrochloride 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)

References

[1] Northrup AB, et al, Discovery of 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 (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met. J Med Chem. 2013 Mar 28;56(6):2294-310. DOI:10.1021/jm301619u
[2] Bhardwaj V, et al. C-Met inhibitor MK-8003 radiosensitizes c-Met-expressing non-small-cell lung cancer cells with radiation-induced c-Met-expression. J Thorac Oncol. 2012 Aug;7(8):1211-7. DOI:10.1097/JTO.0b013e318257cc89
[3] Chandrani Chattopadhyay, et al. Simultaneous inhibition of the HGF/MET and Erk1/2 pathways affect uveal melanoma cell growth and migration. PLoS One. 2014 Feb 13;9(2):e83957. DOI:10.1371/journal.pone.0083957

MK-8033 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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MK-8033 (hydrochloride) Suppliers

China 29 United States 6 Global 35
Haoyuan Chemexpress Co., Ltd.
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1283000-43-0, MK-8033 (hydrochloride)Related Search:


  • MK-8033 (hydrochloride)
  • 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide hydrochloride (1:1)
  • MK-8033 HCl
  • MK8033 HYDROCHLORIDE;MK 8033 HYDROCHLORIDE
  • 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 hydrochloride
  • 1283000-43-0
  • C25H21N5O3SHCl