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MRTX849 (Adagrasib)

Cat. No. M9428
MRTX849 (Adagrasib) Structure
Synonym:

Adagrasib; MRTX-849

Size Price Availability Quantity
5mg USD 67.5  USD75 In stock
10mg USD 103.5  USD115 In stock
25mg USD 225  USD250 In stock
50mg USD 405  USD450 In stock
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Quality Control
Biological Activity

MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor. MRTX849 (Adagrasib) maximizes inhibition by irreversibly locking the KRAS molecule in its inactive state, thereby preventing tumor cell growth which results in tumor cell death. MRTX849 (Adagrasib) exhibited significantly improved half-life and penetration into the tumor, shutting down KRAS signaling for the entire dosing interval, and showing a higher degree of antitumor activity than previous KRAS mutant-selective inhibitors.

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 604.12
Formula C32H35ClFN7O2
CAS Number 2326521-71-3
Purity 99.48%
Solubility DMSO ≥ 30 mg/mL
Storage -20°C, dry, sealed
References

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Pat lents.
Hallin J, et al. Cancer Discov. 2020 Jan;10(1):54-71. PMID: 31658955.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MRTX849 (Adagrasib), Adagrasib; MRTX-849 supplier, Ras, inhibitors

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