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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
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10 mM * 1 mL/2 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3112.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥2100.0 |
| 规格： | 5 mg | 产品价格： | ￥3000.0 |
| 规格： | 10 mg | 产品价格： | ￥5100.0 |
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MK-8033
CAS No. : 1001917-37-8
MCE 国际站：MK-8033
产品活性：MK-8033 是一种具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂 (IC50s: 1 nM (c-Met)，7 nM (Ron))，优先结合活化的激酶构象 (activated kinase conformation)。MK-8033 可用于癌症的研究，例如乳腺癌，膀胱癌、非小细胞肺癌 (NSCLC)。
研究领域：Protein Tyrosine Kinase/RTK
作用靶点：c-Met/HGFR
In Vitro: MK-8033 (Compound 11r, 10 μM) displayed 31% inhibition of CYP3A4 (cytochrome P450 3A4).
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.
MK-8033 (1-10 μM, 72 h) inhibits GTL-16 cell proliferation (IC50: 0.58 μM).
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.
MK-8033 (0.1-10 μM, 2 h) reduces the phosphorylation of c-Met, ERK, and Akt in EBC-1 and H1993 cells.
MK-8033 (1 μM, 1 h) sensitizes EBC-1 and H1993 cells (high c-Met-expressing) to radiation.
MK-8033 (10 μM, 6 h) enhances γ-H2Ax levels in A549 cells compared to double irradiation and decreases in DNA repair.
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.
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.
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).
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文献和实验Typical 5'-kinase labeling reactions included the DNA to be labeled, [[gamma]]-32-P-rATP, T4 polynucleotide kinase, and buffer (3). After incubation at 37degC, reactions are heat inactivated by incubation at 80degC. Portions
, dry 5. block half of the plate (with platelets) by PBS-BSA 1% and coat another half by glycine (x1) - BSA for 1 hour at 37ѓC 6. wash 3 times in PBS-tween 20, dry 7. incubated at 37ѓc for 1 hour with a 1:1000 dilution of rat IgG2a anti-mouse kappa
E L I S A w i t h p l a t e l e t s
2 % for 5 min, RT wash 3 times in PBS-tween 20, dry block half of the plate (with platelets) by PBS-BSA 1% and coat another half by glycine (x1) - BSA for 1 hour at 37ѓC wash 3 times in PBS-tween 20, dry incubated at 37 ѓc
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