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MK-8353

Cat. No. M9803

All AbMole products are for research use only, cannot be used for human consumption.

MK-8353 Structure
Synonym:

SCH900353

Size Price Availability Quantity
1mg USD 70  USD70 In stock
5mg USD 190  USD190 In stock
10mg USD 340  USD340 In stock
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Quality Control & Documentation
Biological Activity

MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK1/2 inhibitor, with IC50 values of 23.0 nM and 8.8 nM, respectively. MK-8353 is a weak inhibitor of hERG current, producing 16% inhibition at 0.6 μM. The IC50 values for inhibiting cell prolifertion are 371, 51, and 23 nM in A2058, HT-29, and Colo-205 cells respectively. MK-8353 also shows potent antitumor activity against various cancer cell lines, such Malme-3M cells (Melanoma), Colo-205 cells (Colon), NCI-H292 cells (Lung), A-549 cells (NSCLC), 8505C cells (Thyroid), SW-626 cells (Ovarian), with EC50s of 21 nM, 19 nM, 130 nM, 230 nM, 210 nM, 108 nM.

In vivo, MK-8353 (60 mg/kg, p.o., bid (twice daily)) causes at least 50% tumor growth inhibition or regression in 83% of the animal models bearing different tumor cells.

Chemical Information
Molecular Weight 691.84
Formula C37H41N9O3S
CAS Number 1184173-73-6
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Sobhana Babu Boga, et al. ACS Med Chem Lett. MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology

[2] Stergios J Moschos, et al. JCI Insight. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors

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Keywords: MK-8353, SCH900353 supplier, ERK, inhibitors, activators

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