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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
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 355.39
Formula C21H17N5O
CAS Number 1695533-89-1
Solubility (25°C) DMSO 55 mg/mL
Storage 2-8°C, protect from light
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] 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




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


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