2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. BI-2865

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM).

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

CAS No. : 2937327-93-8

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Customer Review

Based on 11 publication(s) in Google Scholar

BI-2865 Related Antibodies

Top Publications Citing Use of Products

    BI-2865 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 3;85(5):956-972.  [Abstract]

    Growth inhibition of MIA PaCa-2 cells by ADT-007 vs. BI-2865 or AMG-510 (0-10 μM) as determined by CTG assay following 72-h treatment.

    BI-2865 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Jun 1:591:216904.  [Abstract]

    Dose-response of four cancer cell lines with the three resistant variants to MRTX1133 and BI-2865 (0-10 μM) treatment over 3 days.

    BI-2865 purchased from MedChemExpress. Usage Cited in: Mol Syst Biol. 2025 Feb;21(2):107-125.  [Abstract]

    Comparison of SIMPL2 and NanoBiT in evaluating the KRAS inhibitor BI2865 (0-1 μM). SIMPL2 stable cells expressing IC-β9-KRAS(WT)/β10-IN-RBD were simultaneously treated with both doxycycline and BI2865 for 5 h at the indicated concentrations followed by luminescence measurement. In contrast, the expression of SmBiT-KRAS(WT)/LgBiT-RBD was induced for 16 h in NanoBiT stable cells, followed by BI2865 treatment. Data are presented as mean ± s.d. with n = 4 biological replicates and were fitted into a four-parameter inhibitor-response model

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    Description

    BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM)[1].

    In Vitro

    BI-2865 is a derivative with a prolinol substituent and a pyrimidine linker. BI-2865 has direct ionic interaction with E62, and a water-mediated hydrogen bond network with the side chain of R68 and the main chain carbonyl of Q61, as shown in Co-crystal structures of BI-2865 bound to KRAS[1].
    BI-2865 (5 days) inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells in the presence of IL-13, with a mean IC50 of roughly 140 nM[1].

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

    BI-2865 Related Antibodies
    Molecular Weight

    465.57

    Formula

    C23H27N7O2S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(O[C@@H](C)[C@@H]5CCCN5C)=CC=N4)=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 : 250 mg/mL (536.98 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 2.1479 mL 10.7395 mL 21.4790 mL
    5 mM 0.4296 mL 2.1479 mL 4.2958 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.

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.16%

    SDS (251 KB)

    COA (257 KB) HNMR (171 KB) RP-HPLC (234 KB) MS (69 KB)

    Handling Instructions (2659 KB)
    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 2.1479 mL 10.7395 mL 21.4790 mL 53.6976 mL
    5 mM 0.4296 mL 2.1479 mL 4.2958 mL 10.7395 mL
    10 mM 0.2148 mL 1.0740 mL 2.1479 mL 5.3698 mL
    15 mM 0.1432 mL 0.7160 mL 1.4319 mL 3.5798 mL
    20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6849 mL
    25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1479 mL
    30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7899 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3424 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
    80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
    100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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    BI-2865 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.

    Keywords:

    BI-28652937327-93-8BI2865BI 2865RasCancerKRAS inhibitorBaF3 cellKRAS mutantInhibitorinhibitorinhibit

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