VX-689
MK-5108 (VX-689)
CAS: 1010085-13-8
Molecular Formula: C22H21ClFN3O3S
VX-689 - Names and Identifiers
VX-689 - Physico-chemical Properties
| Molecular Formula | C22H21ClFN3O3S |
| Molar Mass | 461.94 |
| Density | 1.429 |
| Boling Point | 637.6±65.0 °C(Predicted) |
| pKa | 4.41±0.44(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | MK-5108 inhibition of Aurora-A activity, ATP competitive inhibitors. MK-5108 was highly selective for Aurora-A compared to other protein kinases. MK-5108 inhibition of only one kinase (TrkA), the selectivity of <100 times. MK-5108 inhibition of Aurora-A was higher than that of mln8054. Consistent with the induction of phh3-positive cells, MK-5108 of the induced cells accumulated in phase G2-M. MK-5108 inhibition of tumor cell proliferation, including HCC1143, AU565, MCF-7, HCC1806 and CAL85-1,IC50 were 0.42 μm, 0.45 μm, 0.52 μm, 0.56 μm and 0.74 μm, respectively. MK-5108 acts on LEIO285, LEIO505 and SK-LSM1 cells to reduce cell viability in a dose-dependent manner, with an IC50 of approximately 100 nM. After 48 and 72 hours of MK-5108 treatment, the ratio of cells in G2/M phase was increased. Caspase MK-5108 activity was significantly increased at the same time point compared to the DMSO treated control group. LEIO505 cells were exposed to MK-5108 for 24 hours instead of 48 or 72 hours to allow cells to accumulate in the G2/M phase. MK-5108 the ULMS cell line was stopped at the M phase, and MK-5108 decreased the IC50 value of gemcitrate on LEIO285 cells, but increased the IC50 value of gemcitrate on LEIO505 and SK-LMS1 cells. MK-5108 inhibited Aurora-A of the activity and was a competitive inhibitor of ATP. MK-5108 was highly selective for Aurora-A compared to other protein kinases. MK-5108 inhibition of only one kinase (TrkA), the selectivity of <100 times. MK-5108 inhibition of Aurora-A was higher than that of mln8054. Consistent with the induction of phh3-positive cells, MK-5108 of the induced cells accumulated in phase G2-M. MK-5108 inhibition of tumor cell proliferation, including HCC1143, AU565, MCF-7, HCC1806 and CAL85-1,IC50 0.42 μm, 0.45 μm, 0.52 μm, 0.56 μm and 0.74 μm. MK-5108 acts on LEIO285, LEIO505 and SK-LSM1 cells to reduce cell viability in a dose-dependent manner, with an IC50 of approximately 100 nM. After 48 and 72 hours of MK-5108 treatment, the ratio of cells in G2/M phase was increased. Caspase MK-5108 activity was significantly increased at the same time point compared to the DMSO treated control group. LEIO505 cells were exposed to MK-5108 for 24 hours instead of 48 or 72 hours to allow cells to accumulate in the G2/M phase. MK-5108 the ULMS cell line was stopped at the M phase, and MK-5108 decreased the IC50 value of gemcitrate on LEIO285 cells, but increased the IC50 value of gemcitrate on LEIO505 and SK-LMS1 cells. |
| In vivo study | MK-5108 pHH3 positive cells were induced at doses of 16 mg/kg and 32 mg/kg. Plasma concentrations were 1.7 μm and 4.4 μm at 8 mg/kg and 16 mg/dose treatments MK-5108. The tumor and skin tissues were treated with MK-5108, pHH3 production was induced after 2 hours, and the highest amount was reached by 4 hours. MK-5108 at doses of 15 mg/kg and 30 mg/kg significantly inhibited tumor growth, the percentage ratio of mean tumor volume change in the experimental group to the volume change in the control group (%T/C). Treatment was 10% and − 6% on day 11 and 17% and 5% on day 18. MK-5108 according to the above two doses, the drug resistance is good, and the weight loss of the experimental animals is very small. MK-5108 intermittent treatment of SW48 tumor bearing nude mice, with significant anticancer activity, MK-5108 at 15 mg/kg and 45 mg/kg dose treatment inhibited tumor growth, this effect is dose-dependent, treatment day 10% T/C were 35% and 7%, On treatment day 27, the% T/C was 58% and 32%, respectively. MK-5108 pHH3 positive cells were induced at doses of 16 mg/kg and 32 mg/kg. Plasma concentrations were 1.7 μm and 4.4 μm at 8 mg/kg and 16 mg/dose treatments MK-5108. The tumor and skin tissues were treated with MK-5108, pHH3 production was induced after 2 hours, and the highest amount was reached by 4 hours. MK-5108 at doses of 15 mg/kg and 30 mg/kg significantly inhibited tumor growth, the percentage ratio of mean tumor volume change in the experimental group to the volume change in the control group (%T/C). Treatment was 10% and − 6% on day 11 and 17% and 5% on day 18. MK-5108 according to the above two doses, the drug resistance is good, and the weight loss of the experimental animals is very small. MK-5108 intermittent treatment of SW48 tumor bearing nude mice, with significant anticancer activity, MK-5108 at 15 mg/kg and 45 mg/kg dose treatment inhibited tumor growth, this effect is dose-dependent, the% T/C was 35% and 7% on day 10 of treatment and 58% and 32% on day 27 of treatment. |
VX-689 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.165 ml | 10.824 ml | 21.648 ml |
| 5 mM | 0.433 ml | 2.165 ml | 4.33 ml |
| 10 mM | 0.216 ml | 1.082 ml | 2.165 ml |
| 5 mM | 0.043 ml | 0.216 ml | 0.433 ml |
Last Update：2024-01-02 23:10:35
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CAS: 1010085-13-8
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Product Name: MK-5108 (VX-689) Visit Supplier Webpage Request for quotation
CAS: 1010085-13-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1010085-13-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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