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MK-8353

Cat. No. M9803
MK-8353 Structure
Synonym:

SCH900353

Size Price Availability Quantity
5mg USD 260  USD260 In stock
10mg USD 390  USD390 In stock
25mg USD 790  USD790 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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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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  Catalog
Abmole Inhibitor Catalog




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


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