Art. -Nr.: HY-148278

BI-0474

Name: BI-0474
Brand: MedChemExpress
SKU: HY-148278
Price: 150.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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BI-0474 is a potent KRAS^G12C inhibitor with an IC₅₀ value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

The BI-0474 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Reinheit : 99.83%
CAS. Nr.: 2750570-55-7
Formel: C₃₀H₃₇N₉O₂S
Molecular Weight:587.74

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BI-0474 Chemical Structure

CAS. Nr.: 2750570-55-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KRAS-SOS1

7.0 nM (IC₅₀)

Alle Ras Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LS-513	EC₅₀	>4 μM Compound: 23; BI-0474	Antiproliferative activity against human LS-513 cells harboring KRAS G12D mutant incubated for 5 days by celltiter glo luminescent assay Antiproliferative activity against human LS-513 cells harboring KRAS G12D mutant incubated for 5 days by celltiter glo luminescent assay	[PMID: 36300829]
NCI-H358	EC₅₀	26 nM Compound: 23; BI-0474	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay	[PMID: 36300829]

In Vitro

BI-0474 (1-10,000 nM; 3 days) shows potent antiproliferative activity of 26 nM on NCI-H358 cells carrying a G12C mutation^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

NCI-H358 cells (carrying a G12C mutation)
Concentration:

1-10,000 nM
Incubation Time:

3 days
Result:

Inhibited proliferation of NCI-H358 cells with an EC₅₀ of 26 nM.

In Vivo

BI-0474 (40 mg/kg; i.p.; single daily for 3 days) shows anti-tumor efficacy and pharmacodynamic biomarker modulation in an NCI-H358 cell line-derived non-small cell lung cancer xenograft model^[1].

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

Animal Model:

NMRI nude mice (NCI-H358 cell line-derived non-small cell lung cancer xenograft model)^[1].
Dosage:

40 mg/kg
Administration:

Intraperitoneal administration; single daily for 3 days
Result:

Led to induction of programmed cell death in this xenograft model.

Chemical Information

CAS. Nr. 2750570-55-7
Appearance Solid
Molecular Weight 587.74
Formel C₃₀H₃₇N₉O₂S
Color White to off-white
SMILES

N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(N5[C@@H](C)CN(C)CC5)=CC(N6CCN(C(C=C)=O)CC6)=C4)=NO3)CCC2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (170.14 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

1.7014 mL

8.5072 mL

17.0143 mL

5 mM

0.3403 mL

1.7014 mL

3.4029 mL

10 mM

0.1701 mL

0.8507 mL

1.7014 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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)
Handling Instructions (2659 KB)

Verweise

[1]. Bröker J, et al. Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor. J Med Chem. 2022 Oct 27. [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	1.7014 mL	8.5072 mL	17.0143 mL	42.5358 mL
	5 mM	0.3403 mL	1.7014 mL	3.4029 mL	8.5072 mL
	10 mM	0.1701 mL	0.8507 mL	1.7014 mL	4.2536 mL
	15 mM	0.1134 mL	0.5671 mL	1.1343 mL	2.8357 mL
	20 mM	0.0851 mL	0.4254 mL	0.8507 mL	2.1268 mL
	25 mM	0.0681 mL	0.3403 mL	0.6806 mL	1.7014 mL
	30 mM	0.0567 mL	0.2836 mL	0.5671 mL	1.4179 mL
	40 mM	0.0425 mL	0.2127 mL	0.4254 mL	1.0634 mL
	50 mM	0.0340 mL	0.1701 mL	0.3403 mL	0.8507 mL
	60 mM	0.0284 mL	0.1418 mL	0.2836 mL	0.7089 mL
	80 mM	0.0213 mL	0.1063 mL	0.2127 mL	0.5317 mL
	100 mM	0.0170 mL	0.0851 mL	0.1701 mL	0.4254 mL

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BI-0474

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