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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
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 691.84
Formula C37H41N9O3S
CAS Number 1184173-73-6
Purity >99%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
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 2017




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

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