1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. BI-2493

BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research.

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

BI-2493

BI-2493 Chemical Structure

CAS No. : 2937344-16-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 4 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research[1].

IC50 & Target

K-Ras WT

 

In Vitro

BI-2493 (0-10 μM, 72 h) inhibits the proliferation of KRAS mutant cancer cell lines in a concentration-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: ASPC1 cells (G12D), HPAC cells (G12D), H727 cells (G12V) (BaF3 cells transduced with a virus derived from plasmids expressing KRAS G12D or G12V mutants)
Concentration: 0, 100 nM, 1000 nM, 10000 nM
Incubation Time: 72 h
Result: Effectively inhibited the proliferation of cancer cells ASPC1 (G12D), HPAC (G12D), and H727 (G12V)
In Vivo

BI-2493 (90 mg/kg, p.o., twice daily for 21 days) exhibits tumor-suppressive activity in LS513/GP2d/HPAC/SW620/MIAPACA2-derived xenograft NMRI mice models[1].

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

Animal Model: LS513/GP2d/HPAC/SW620/MIAPACA2-derived xenograft NMRI mice models
Dosage: 90 mg/kg
Administration: Oral gavage (p.o.), twice daily for 21 days
Result: Reduced tumor growth in mice carrying KRAS G12C, G12D, G12V, and A146V mutation models, without causing significant toxicity to the mice.
Molecular Weight

461.58

Formula

C24H27N7OS

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

N#CC1=C(N)SC2=C1[C@]3(CCC2)C4=C(CCC3)C(C5=NC(N6[C@H](CNCC6)C)=NC=C5)=NO4

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 : 50 mg/mL (108.32 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 2.1665 mL 10.8324 mL 21.6647 mL
5 mM 0.4333 mL 2.1665 mL 4.3329 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
=
Concentration
×
Volume
×
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: ≥ 1.25 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 99.79%

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 2.1665 mL 10.8324 mL 21.6647 mL 54.1618 mL
5 mM 0.4333 mL 2.1665 mL 4.3329 mL 10.8324 mL
10 mM 0.2166 mL 1.0832 mL 2.1665 mL 5.4162 mL
15 mM 0.1444 mL 0.7222 mL 1.4443 mL 3.6108 mL
20 mM 0.1083 mL 0.5416 mL 1.0832 mL 2.7081 mL
25 mM 0.0867 mL 0.4333 mL 0.8666 mL 2.1665 mL
30 mM 0.0722 mL 0.3611 mL 0.7222 mL 1.8054 mL
40 mM 0.0542 mL 0.2708 mL 0.5416 mL 1.3540 mL
50 mM 0.0433 mL 0.2166 mL 0.4333 mL 1.0832 mL
60 mM 0.0361 mL 0.1805 mL 0.3611 mL 0.9027 mL
80 mM 0.0271 mL 0.1354 mL 0.2708 mL 0.6770 mL
100 mM 0.0217 mL 0.1083 mL 0.2166 mL 0.5416 mL
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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-2493
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