Cat. No.: HY-132966

ASP2453

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

ASP2453 is a potent, selective and orally active KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC₅₀ value of 40 nM.

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Pureté: 98.28%
CAS No.: 2241719-73-1
Formule: C₄₀H₄₈F₃N₇O₄
Masse moléculaire:747.85

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

ASP2453 Chemical Structure

CAS No.: 2241719-73-1

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

KRas G12C

40 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Ras :

Voir tous les produits spécifiques à Isoform ERK :

In Vitro

ASP2453 (0.1 nM-1 μM, 2 h-6 days) inhibits KRAS G12C-mediated phosphorylation of ERK in cell NCI-H1373 with an IC₅₀ of 2.5 nM, inhibits proliferations of KRAS G12C mutated cells, while having no effect on KRAS wild-type or other KRAS mutant cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

NCI-H1373, MIA PaCa-2, NCI-H358, NCI-H23, NCI-H1792, LU65
Concentration:

0.1 nM-1 μM
Incubation Time:

6 days
Result:

Inhibited the cell growth.

In Vivo

ASP2453 (5-30 mg/kg, po, once daily for 30 days) exhibits antitumor activity in mouse xenograft models such as MIA PaCa-2 and LXFA592^[1].

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

Animal Model:

LXFA592 xenograft mouse models^[1]
Dosage:

5-30 mg/kg
Administration:

po, once daily for 30 days
Result:

Inhibited the tumor growth.

Chemical Information

CAS No. 2241719-73-1
Appearance Solid
Masse moléculaire 747.85
Formule C₄₀H₄₈F₃N₇O₄
Color White to yellow
SMILES

C=CC(N1CC2(CCN(C3=C4C=C(C5CC5)C(C6=C(C)C=CC7=C6C=NN7)=C(OCC(F)(F)F)C4=NC(OC8CCN(CCCOC)CC8)=N3)CC2)C1)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Cell

Targeting Ras-, Rho-, and Rab-family GTPases via a conserved cryptic pocket. [Abstract]

2024 Oct 31;187(22):6379-6392.e17. PMID: 39255801
iScience

Serum SOS1 as a prognostic biomarker and therapeutic target for progressive liver disease. [Abstract]

2026 Jun 17;29(7):116430. PMID: 42369045

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (334.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3372 mL

6.6858 mL

13.3717 mL

5 mM

0.2674 mL

1.3372 mL

2.6743 mL

10 mM

0.1337 mL

0.6686 mL

1.3372 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.08 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Nakayama A, et al. Characterisation of a novel KRAS G12C inhibitor ASP2453 that shows potent anti-tumour activity in KRAS G12C-mutated preclinical models. Br J Cancer. 2021 Nov 18. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.3372 mL	6.6858 mL	13.3717 mL	33.4292 mL
	5 mM	0.2674 mL	1.3372 mL	2.6743 mL	6.6858 mL
	10 mM	0.1337 mL	0.6686 mL	1.3372 mL	3.3429 mL
	15 mM	0.0891 mL	0.4457 mL	0.8914 mL	2.2286 mL
	20 mM	0.0669 mL	0.3343 mL	0.6686 mL	1.6715 mL
	25 mM	0.0535 mL	0.2674 mL	0.5349 mL	1.3372 mL
	30 mM	0.0446 mL	0.2229 mL	0.4457 mL	1.1143 mL
	40 mM	0.0334 mL	0.1671 mL	0.3343 mL	0.8357 mL
	50 mM	0.0267 mL	0.1337 mL	0.2674 mL	0.6686 mL
	60 mM	0.0223 mL	0.1114 mL	0.2229 mL	0.5572 mL
	80 mM	0.0167 mL	0.0836 mL	0.1671 mL	0.4179 mL
	100 mM	0.0134 mL	0.0669 mL	0.1337 mL	0.3343 mL

Keywords

ASP2453

2 Cited Publications

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ASP2453

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KRAS Targeted Compound Library

Publications Citing Use of MedChemExpress (MCE) ASP2453

Voir tous les produits spécifiques à Isoform Ras

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ASP2453 Related Classifications

HY-132966 Related Classifications