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Temuterkib

Cat. No. M11529
Temuterkib Structure
Synonym:

LY3214996

Size Price Availability Quantity
2mg USD 130  USD130 In stock
5mg USD 230  USD230 In stock
10mg USD 355  USD355 In stock
25mg USD 690  USD690 In stock
50mg USD 1300  USD1300 In stock
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Quality Control & Documentation
Biological Activity

Temuterkib (LY3214996) is a selective, novel erK1/2 inhibitor with an IC50 of 5 nM against ERK1 and ERK2. It can effectively inhibit intracellular P-RSK1 in cancer cell lines with BRAF and RAS mutations. Temuterkib has strong antitumor activity in cancer models with altered MAPK pathways.

Chemical Information
Molecular Weight 453.56
Formula C22H27N7O2S
CAS Number 1951483-29-6
Solubility (25°C) DMSO ≥ 20 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.

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  Catalog
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Keywords: Temuterkib, LY3214996 supplier, ERK, inhibitors, activators


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