| Identification | Back Directory | [Name]
MK-8033 (hydrochloride) | [CAS]
1283000-43-0 | [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) | [Molecular Formula]
C25H22ClN5O3S | [MDL Number]
MFCD28167721 | [MOL File]
1283000-43-0.mol | [Molecular Weight]
507.99 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [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 |
|
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|