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MRTX849 acid

Cat. No. M21503
MRTX849 acid  Structure
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Biological Activity

MRTX849 acid can be used to synthesize PROTAC LC-2. LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM).

Chemical Information
Molecular Weight 662.15
Formula C34H37ClFN7O4
CAS Number 2561529-96-0
Solubility (25°C) N/A
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.


[1] Matthew R Pincus, et al. Biomedicines. Peptides That Block RAS-p21 Protein-Induced Cell Transformation

[2] Lamei Huang, et al. Signal Transduct Target Ther. KRAS mutation: from undruggable to druggable in cancer

[3] Robert Roskoski Jr. Pharmacol Res. Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS

[4] Mark M Awad, et al. N Engl J Med. Acquired Resistance to KRASG12C Inhibition in Cancer

[5] Rajwanth Veluswamy, et al. J Mol Diagn. KRAS G12C-Mutant Non-Small Cell Lung Cancer: Biology, Developmental Therapeutics, and Molecular Testing

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Keywords: MRTX849 acid supplier, Ras, inhibitors, activators

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