AMG 510

SKU: orb1298716

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Description

Sotorasib (AMG-510) is a selective, covalent inhibitor that targets the inactive, GDP-bound form of the KRAS G12C mutant. It potently suppresses oncogenic KRAS signaling and has demonstrated antitumor efficacy in both cellular assays and in vivo models, supporting its use in cancer research.

Research Area

Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	2296729-00-3
MW	560.6
Purity	>98%
Formula	C₃₀H₃₀F₂N₆O₃
SMILES	O=C1N=C(C=2C=C(F)C(=NC2N1C=3C(=NC=CC3C)C(C)C)C=4C(F)=CC=CC4O)N5CCN(C(=O)C=C)CC5C
Target	GTPase
Solubility	Soluble in DMSO (up to 25 mg/ml)

Bioactivity

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Target IC50	KRas (G12C) (CLM22 organoids):10.95 μM\|KRas (G12C) (CWH22 organoids):12.07 μM
In Vivo	METHODS: To assay antitumor activity in vivo, Sotorasib (3-100 mg/kg) was orally administered once daily for four weeks to athymic nude mice bearing the human pancreatic cancer tumor MIA PaCa-2 T2 or the human lung cancer tumor NCI-H358. RESULTS: Sotorasib significantly inhibited the growth of MIA PaCa-2 T2 and NCI-H358 tumors at all doses, and tumor regression was observed at higher doses. METHODS: To assay antitumor activity in vivo, Sotorasib (30 mg/kg in 0.5% sodium carboxymethylcellulose, administered by gavage once daily) and Cisplatin (4 mg/kg in 0.9% saline, intraperitoneally every two days) were administered to Balb/C nude mice harboring human lung cancer tumors. RESULTS: Tumor shrinkage in the combination group was more than twice that of the single-administration group. Read more...
In Vitro	METHODS: Twenty-two tumor cells were treated with Sotorasib (0-10 μM) for 72 h. Cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. RESULTS: Sotorasib impaired the growth of all KRAS G12C cell lines except SW1573, with IC50 values ranging from 0.004-0.032 μM. non-KRAS G12C cell lines were sensitive to Sotorasib, with an IC50 >7.5 μM. METHODS: KRAS G12C mutant tumor cells were treated with Sotorasib (100 nM) for 4-72 h, and the expression levels of target proteins were detected using Western Blot method. RESULTS: Sotorasib rapidly inhibited KRAS downstream signaling, but p-ERK levels returned to 75% of the baseline level at 72 h. Sotorasib was also shown to rapidly inhibit KRAS downstream signaling. Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Sotorasib

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Compound Identifiers

PubChem CID

138461166 ↗

Key Properties

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No computed properties available.

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AMG 510 (orb1298716)

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Purity:	99.76% (May vary between batches)
CAS Number:	2252403-56-6
MW:	560.594
Formula:	C₃₀H₃₀F₂N₆O₃

Purity:	>98% (HPLC)
CAS Number:	2296729-00-3
MW:	560.59
Formula:	C??H??F?N?O?

Purity:	>98% (HPLC)
CAS Number:	2252403-56-6
MW:	560.59
Formula:	C??H??F?N?O?

AMG 510

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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AMG 510 (orb1298716)

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