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MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $51 | In Stock | |
5 mg | $120 | In Stock | |
10 mg | $178 | In Stock | |
25 mg | $301 | In Stock | |
50 mg | $451 | In Stock | |
100 mg | $663 | In Stock | |
500 mg | $1,390 | In Stock |
Description | MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer. |
In vitro | MDL-800 increased SIRT6 deacetylase activity with an EC50 value of 11.0 ± 0.3 μM; MDL-800 (10-50 μM) induced dose-dependent deacetylation of histone H3 in 12 NSCLC cell lines. Treatment with MDL-800 dose dependently inhibited the proliferation of 12 NSCLC cell lines with IC50 values ranging from 21.5 to 34.5 μM. The antiproliferation effect of MDL-800 was significantly diminished by SIRT6 knockout. Treatment with MDL-800 induced remarkable cell cycle arrest at the G0/G1 phase in NSCLC HCC827 and PC9 cells. Furthermore, MDL-800 (25, 50 μM) enhanced the antiproliferation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in osimertinib-resistant HCC827 and PC9 cells as well as in patient-derived primary tumor cells, and suppressed mitogen-activated protein kinase (MAPK) pathway.[1] |
In vivo | In HCC827 cell-derived xenograft nude mice, intraperitoneal administration of MDL-800 (80 mg · kg-1 · d-1, for 14 days) markedly suppressed the tumor growth, accompanied by enhanced SIRT6-dependent histone H3 deacetylation and decreased p-MEK and p-ERK in tumor tissues.[1] |
Alias | MDL800, MDL 800 |
Molecular Weight | 626.3 |
Formula | C21H16BrCl2FN2O6S2 |
Cas No. | 2275619-53-7 |
Storage | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (71.85 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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