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
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
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.
N-Bromosuccinimide Price
- Product number
- CS-1849
- Product name
- MK-8033hydrochloride
- Purity
- 99.70%
- Packaging
- 5mg
- Price
- $456
- Updated
- 2021/12/16
- Product number
- CS-1849
- Product name
- MK-8033hydrochloride
- Purity
- 99.70%
- Packaging
- 10mg
- Price
- $696
- Updated
- 2021/12/16
- Product number
- orb611564
- Product name
- MK-8033 hydrochloride
- Packaging
- 100mg
- Price
- $1654.1
- Updated
- 2021/12/16
- Product number
- CS-1849
- Product name
- MK-8033hydrochloride
- Purity
- 99.70%
- Packaging
- 50mg
- Price
- $1656
- Updated
- 2021/12/16
- Product number
- orb611564
- Product name
- MK-8033 hydrochloride
- Packaging
- 250mg
- Price
- $3282.7
- Updated
- 2021/12/16
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
MK-8033 (hydrochloride) Suppliers
- Tel
- +1-800-259-7612
- Fax
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- United States
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- +17819995354
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