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AMG-510 (Sotorasib)

Cat. No. M9356
AMG-510 (Sotorasib) Structure
Synonym:

Sotorasib; AMG510

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 80  USD80 In stock
10mg USD 140  USD140 In stock
25mg USD 300  USD300 In stock
50mg USD 480  USD480 In stock
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Quality Control
Biological Activity

AMG-510 (Sotorasib) selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant.

In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. AMG 510 (orally, once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer.

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 560.59
Formula C30H30F2N6O3
CAS Number 2296729-00-3
Purity 99.90%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Shannon S Zhang, et al. Spotlight on Sotorasib (AMG 510) for KRAS G12C Positive Non-Small Cell Lung Cancer

[2] David S Hong, et al. KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors

[3] No authors listed. Cancer Discov. AMG 510 Shows Activity beyond NSCLC

[4] Brian A Lanman, et al. Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors

[5] Jude Canon, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AMG-510 (Sotorasib), Sotorasib; AMG510 supplier, Ras, inhibitors

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