1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. BI-0474

BI-0474 is a potent KRASG12C 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.

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

BI-0474 Chemical Structure

BI-0474 Chemical Structure

CAS No. : 2750570-55-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 2586 In-stock
Solution
10 mM * 1 mL in DMSO USD 2586 In-stock
Solid
1 mg USD 650 In-stock
5 mg USD 2000 In-stock
10 mg USD 3000 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

BI-0474 is a potent KRASG12C 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[1].

IC50 & Target

KRAS-SOS1

7.0 nM (IC50)

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.
Molecular Weight

587.74

Formula

C30H37N9O2S

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7014 mL 8.5072 mL 17.0143 mL
5 mM 0.3403 mL 1.7014 mL 3.4029 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.83%

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. 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 Related Classifications

Help & FAQs
  • 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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BI-0474
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