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  3. Sotorasib

Sotorasib (Synonyms: AMG-510)

Cat. No.: HY-114277 Purity: 99.41%
Handling Instructions

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.

For research use only. We do not sell to patients.

Sotorasib Chemical Structure

Sotorasib Chemical Structure

CAS No. : 2296729-00-3

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10 mM * 1 mL in DMSO USD 111 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

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Description

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors[1][2].

IC50 & Target[1]

KRAS(G12C)

 

In Vitro

In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines[2].
Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay [3]

Cell Line: NCI-H358 and MIA PaCa-2 cells
Concentration: 1-10 μM
Incubation Time: 72 hours
Result: Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC50≈0.006 μM and 0.009 μM respectively).
In Vivo

In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

560.59

Formula

C₃₀H₃₀F₂N₆O₃

CAS No.
SMILES

O=C(C=C)N1C[[email protected]](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (89.19 mM; Need ultrasonic)

H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7838 mL 8.9192 mL 17.8383 mL
5 mM 0.3568 mL 1.7838 mL 3.5677 mL
10 mM 0.1784 mL 0.8919 mL 1.7838 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 5 mg/mL (8.92 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 99.60%

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Keywords:

SotorasibAMG-510AMG510AMG 510RasNSCLCKRASG12Canti-tumourcovalentregressionmutationGDP-boundphosphorylationInhibitorinhibitorinhibit

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