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  3. AMG-510

AMG-510 

Cat. No.: HY-114277 Purity: 99.60%
Handling Instructions

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor, which locks KRAS G12C in an inactive GDP-bound state. AMG-510 selectively targets the KRAS p.G12C mutant and shows anti-tumor activity.

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

AMG-510 Chemical Structure

AMG-510 Chemical Structure

Size Price Stock Quantity
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
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor, which locks KRAS G12C in an inactive GDP-bound state. AMG-510 selectively targets the KRAS p.G12C mutant and shows anti-tumor activity[1][2].

IC50 & Target[1]

KRAS(G12C)

 

In Vitro

In cellular assays, 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].

In Vivo

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[3].

Clinical Trial
Molecular Weight

560.59

Formula

C₃₀H₃₀F₂N₆O₃

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 : 125 mg/mL (222.98 mM; Need ultrasonic)

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
AMG-510
Cat. No.:
HY-114277
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