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Rineterkib

Cat. No. M10733
Rineterkib  Structure
Size Price Availability Quantity
5mg USD 225  USD225 In stock
10mg USD 410  USD410 In stock
25mg USD 880  USD880 In stock
50mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

Rineterkib (compound B) is an orally active inhibitor of ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.

Chemical Information
Molecular Weight 578.42
Formula C26H27BrF3N5O2
CAS Number 1715025-32-3
Solubility (25°C) DMSO ≥ 150 mg/mL
Storage 4°C, protect from light, dry
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] Song Y, et al. Genes & Diseases. Targeting RAS–RAF–MEK–ERK signaling pathway in human cancer: Current status in clinical trials

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Keywords: Rineterkib supplier, ERK, inhibitors, activators


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