1. Others GPCR/G Protein MAPK/ERK Pathway
  2. Isotope-Labeled Compounds Ras
  3. Sotorasib-d7

Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). 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 leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC).

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

Sotorasib-d<sub>7</sub> Chemical Structure

Sotorasib-d7 Chemical Structure

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Description

Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). 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 leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC)[1][2][3].

IC50 & Target

KRAS(G12C)

 

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

Molecular Weight

567.64

Formula

C30H23D7F2N6O3

Unlabeled CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(C=C)N1C([2H])([2H])[C@H](C([2H])([2H])[2H])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)C([2H])([2H])C1

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 : ≥ 100 mg/mL (176.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7617 mL 8.8084 mL 17.6168 mL
5 mM 0.3523 mL 1.7617 mL 3.5234 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7617 mL 8.8084 mL 17.6168 mL 44.0420 mL
5 mM 0.3523 mL 1.7617 mL 3.5234 mL 8.8084 mL
10 mM 0.1762 mL 0.8808 mL 1.7617 mL 4.4042 mL
15 mM 0.1174 mL 0.5872 mL 1.1745 mL 2.9361 mL
20 mM 0.0881 mL 0.4404 mL 0.8808 mL 2.2021 mL
25 mM 0.0705 mL 0.3523 mL 0.7047 mL 1.7617 mL
30 mM 0.0587 mL 0.2936 mL 0.5872 mL 1.4681 mL
40 mM 0.0440 mL 0.2202 mL 0.4404 mL 1.1010 mL
50 mM 0.0352 mL 0.1762 mL 0.3523 mL 0.8808 mL
60 mM 0.0294 mL 0.1468 mL 0.2936 mL 0.7340 mL
80 mM 0.0220 mL 0.1101 mL 0.2202 mL 0.5505 mL
100 mM 0.0176 mL 0.0881 mL 0.1762 mL 0.4404 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Sotorasib-d7
Cat. No.:
HY-114277S
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