BI-2865
Based on 12 publication(s) in Google Scholar
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).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.16%
- CAS 番号: 2937327-93-8
- 分子式: C23H27N7O2S
- 分子量:465.57
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 BI-2865
More- Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]
- Cancer Res. 2026 May 27:10.1158/0008-5472.CAN-25-5172. [Abstract]
- Cancer Res. 2025 Mar 3;85(5):956-972. [Abstract]
- Adv Sci (Weinh). 2026 Feb 12:e15654. [Abstract]
- Cancer Lett. 2024 Jun 1:591:216904. [Abstract]
- Mol Syst Biol. 2025 Feb;21(2):107-125. [Abstract]
- Mol Oncol. 2025 Mar 11. [Abstract]
- J Chin Med Assoc. 2026 Feb 1;89(2):140-150. [Abstract]
- bioRxiv. 2026 Feb 20.
- SSRN. 2025 Nov 6.
- bioRxiv. 2025 Aug 2:2025.07.31.667978. [Abstract]
- bioRxiv. 2024 October 04.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
生物活性
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.
化学情報
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CAS 番号 2937327-93-8
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性状 Solid
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分子量 465.57
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分子式 C23H27N7O2S
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Color Light yellow to brown
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SMILES
N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(O[C@@H](C)[C@@H]5CCCN5C)=CC=N4)=NO3)CCC2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Cell
A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213 -
Cancer Res
Targeted KRASG12V Degradation in vivo Elicits Lung Adenocarcinoma Regression with Subsequent Relapse from Dysregulated Proteolysis. [Abstract]2026 May 27:10.1158/0008-5472.CAN-25-5172. PMID: 42200804 -
Cancer Res
A Pan-RAS Inhibitor with a Unique Mechanism of Action Blocks Tumor Growth and Induces Antitumor Immunity in Gastrointestinal Cancer. [Abstract]2025 Mar 3;85(5):956-972. PMID: 39700396
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.
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Adv Sci (Weinh)
Real-Time Visualization of Isoform-Specific RAF-KRAS Interactions in Living Cells Using FRET-BRET Hybrid Biosensors. [Abstract]2026 Feb 12:e15654. PMID: 41674298 -
Cancer Lett
Site-specific mutagenesis screening in KRASG12D mutant library to uncover resistance mechanisms to KRASG12D inhibitors. [Abstract]2024 Jun 1:591:216904. PMID: 38642608
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.
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Mol Syst Biol
A split intein and split luciferase-coupled system for detecting protein-protein interactions. [Abstract]2025 Feb;21(2):107-125. PMID: 39668253
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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Mol Oncol
The atypical KRASQ22K mutation directs TGF-β response towards partial epithelial-to-mesenchymal transition in patient-derived colorectal cancer tumoroids. [Abstract]2025 Mar 11. PMID: 40066744 -
J Chin Med Assoc
Single-cell omics in investigating the effect of CAFs with KRAS overexpression on the malignant progression of anaplastic thyroid cancer. [Abstract]2026 Feb 1;89(2):140-150. PMID: 41486477 -
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bioRxiv
2025 Aug 2:2025.07.31.667978. PMID: 40766426 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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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)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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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