MK-8033 (hydrochloride)
CAS No. : 1283000-43-0
| Size | Price | Stock |
|---|---|---|
| 5mg | $300 | In-stock |
| 10mg | $510 | In-stock |
| 50mg | $1600 | In-stock |
| 100mg | $2560 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-13299A |
| M.Wt: | 507.99 |
| Formula: | C25H22ClN5O3S |
| Purity: | >98 % |
| Solubility: | H2O : 7.14 mg/mL (ultrasonic);DMSO : 5.88 mg/mL (ultrasonic) |
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].
IC50 & Target: IC50: 7 nM (Ron)[1]
In Vitro: MK-8033 hydrochloride (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4)[1].
MK-8033 hydrochloride (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 hydrochloride (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC50: 0.58 μM)[1].
MK-8033 hydrochloride 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 hydrochloride (0.1-10 μM, 2 h) reduces the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells[2].
MK-8033 hydrochloride (1 μM, 1 h) sensitizes EBC-1 and H1993 cells (high c-Met-expressing) to radiation[2].
MK-8033 hydrochloride (10 μM, 6 h) enhances γ-H2Ax levels in A549 cells compared to double irradiation and decreases in DNA repair[2].
MK-8033 hydrochloride (2 μM, 72 h) results in reduced cell proliferation, but modest induction of apoptosis in G-alpha protein mutant UM (uveal melanoma) cells[3].
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].
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