2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. MK-8033

MK-8033 

Cat. No.: HY-13299 Purity: 98.06%
COA Handling Instructions

MK-8033 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 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs).

For research use only. We do not sell to patients.

MK-8033 Chemical Structure

MK-8033 Chemical Structure

CAS No. : 1001917-37-8

Size Price Stock
Solution
10 mM * 1 mL in DMSO USD 502 Ask For Quote & Lead Time
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 502 Ask For Quote & Lead Time
Solid
5 mg USD 456 Ask For Quote & Lead Time
10 mg USD 696 Ask For Quote & Lead Time
50 mg USD 1656 Ask For Quote & Lead Time

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MK-8033 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 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs)[1][2].

IC50 & Target[1]

Ron

7 nM (IC50)

In Vitro

MK-8033 (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4)[1].
MK-8033 (1 μM, 2 h) inhibits phosphorylation of Y1349 of c-Met (IC50: 0.03 μM) in the c-Met dependent gastric cancer cell line GTL-16[1].
MK-8033 (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC50: 0.58 μM)[1].
MK-8033 binds more tightly to phosphorylated c-Met (Kd: 3.2 nM) than to its unphosphorylated counterpart (Kd: 10.4 nM), and inhibits oncogenic c-Met activation loop mutants with IC50s ranging from 0.6 to 1 nM[1].
MK-8033 (0.1-10 μM, 2 h) reduces the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells[2].
MK-8033 (1 μM, 1 h) sensitizes EBC-1 and H1993 cells (high c-Met-expressing) to radiation[2].
MK-8033 (10 μM, 6 h) enhances γ-H2Ax levels in A549 cells compared to double irradiation and decreases in DNA repair[2].
MK-8033 (2 μM, 72 h) results in reduced cell proliferation, but modest induction of apoptosis in G-alpha protein mutant UM (uveal melanoma) cells[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: EBC-1, H1993 cells, A549 and H460 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 2 h
Result: Reduced the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells in a dose-dependent manner.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

471.53

Appearance

Solid

Formula

C25H21N5O3S
CAS No.
SMILES

O=S(NCC1=CC=CC=N1)(CC2=CC=C3C(C(C4=CC(C5=CN(N=C5)C)=CN=C4C=C3)=O)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (97.55 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1208 mL 10.6038 mL 21.2076 mL
5 mM 0.4242 mL 2.1208 mL 4.2415 mL
10 mM 0.2121 mL 1.0604 mL 2.1208 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

MK-80331001917-37-8MK8033MK 8033c-Met/HGFRAnti-anceranti-tumorGTL-16EBC-1H1993radiosensitivityNSCLCsbreast cancerbladder cancerInhibitorinhibitorinhibit

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