MK-8033 NEW
| Price | $98 | $145 | $247 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: MK-8033 | CAS No.: 1001917-37-8 |
| Purity: 97.16% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | MK-8033 |
| Description | MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met). |
| In vitro | MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd: 3.2 nM) than to its unphosphorylated counterpart (Kd = 10.4 nM). Significantly, MK-8033 potently inhibits the kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s: 0.6~1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation (IC50: 582 nM). By contrast, the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitizer the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met-expressing cell lines A549 and H460. However, irradiation of A549 and H460 cells increased the expression of c-Met protein at 30 minutes after the irradiation. Subsequent targeting of this up-regulated c-Met by using MK-8033 followed by a second radiation dose reduced the clonogenic survival of both A549 and H460 cells. MK-8033reduced the levels of radiation-induced phosphorylated (activated) c-Met in A549 cells [2]. |
| In vivo | MK-8033 was orally dosed in GTL-16 tumor xenograft bearing mice. Mice were euthanized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg, essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to the tumor from vehicle-treated mice [1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (97.83 mM) |
| Keywords | bladder cancer | breast cancer | EBC-1 | H1993 | MK 8033 | anti-tumor | Inhibitor | GTL-16 | radiosensitivity | Anti-ancer | MK8033 | NSCLCs | inhibit | c-Met/HGFR | MK-8033 |
| Inhibitors Related | Cabozantinib | Capmatinib 2HCl | SGI-7079 | (±)-Norcantharidin | L-Ascorbic acid 2-phosphate trisodium | Crizotinib | Amuvatinib | Norcantharidin | Cabozantinib S-malate | Capmatinib xHCl | Bacitracin Zinc | Capmatinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hills
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