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KO-947

Cat. No. M10071
KO-947 Structure
Synonym:

KO947; K0947

Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 245  USD245 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

KO-947 is a potent and selective ERK inhibitor with slow dissociation kinetics. KO-947 showed potent inhibition of ERK signaling pathways and proliferation of tumor cells exhibiting dysregulation of MAPK pathway, including mutations in BRAF, NRAS or KRAS. KO-947 also inhibits MAPK signaling and cell proliferation in preclinical models that are resistant to BRAF and MEK inhibitors. KO-947 induces tumor regressions in BRAF or RAS mutated tumor models as well as in tumor models lacking BRAF/RAS mutations but characterized by other dysregulation of the MAPK pathway.

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 355.39
Formula C21H17N5O
CAS Number 1695533-89-1
Purity >97%
Solubility DMSO 55 mg/mL
Storage at -20°C
References

[1] Francis Burrows, et al. AACR. KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumors

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: KO-947, KO947; K0947 supplier, ERK, inhibitors

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