ACBI3
Based on 1 Customer Validation
ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models.
(Pink: K-Ras WT ligand (HY-162960); Blue: VHL ligand (HY-401613); Black: linker (HY-169992)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
The ACBI3 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.
- Pureté : 99.47%
- CAS No.: 2938169-76-5
- Formule: C50H62N14O6S2
- Masse moléculaire:1019.25
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
In Vitro
ACBI3 (0.01-10000 nM, 5 days) exhibits antiproliferative activity in KRAS mutant versus KRASWT cell lines (geometric mean IC50 =478 nM versus 8.3 μM, respectively). ACBI3 exhibits high efflux in the Caco-2 assay in LS513 cells[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KRAS mutant xenograft mouse models[1]
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Dosage:2 mg/kg i.v. or 30 mg/kg s.c. or 30 mg/kg i.p.
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Administration:once a day for 3 days
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Result:Resulted in pronounced tumor regressions with a tumor growth inhibition of 127% in KRAS mutant xenograft mouse models.
Chemical Information
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CAS No. 2938169-76-5
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Appearance Solid
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Masse moléculaire 1019.25
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Formule C50H62N14O6S2
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Color White to yellow
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SMILES
NC(SC1=C2[C@](C3=NC(C4=NC(N5CCCN(CCCCOC(N=N6)=CN6[C@@H](C(C)C)C(N7[C@H](C(N[C@@H](CO)C8=CC=C(C=C8)C9=C(N=CS9)C)=O)C[C@@H](O)C7)=O)C[C@@H]5C)=NC=C4)=NO3)(C)CCC1)=C2C#N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 140 mg/mL (137.36 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Pureté et documentation
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Fiche technique (274 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 0.9811 mL | 4.9056 mL | 9.8111 mL | 24.5278 mL |
| 5 mM | 0.1962 mL | 0.9811 mL | 1.9622 mL | 4.9056 mL | |
| 10 mM | 0.0981 mL | 0.4906 mL | 0.9811 mL | 2.4528 mL | |
| 15 mM | 0.0654 mL | 0.3270 mL | 0.6541 mL | 1.6352 mL | |
| 20 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2264 mL | |
| 25 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL | 0.9811 mL | |
| 30 mM | 0.0327 mL | 0.1635 mL | 0.3270 mL | 0.8176 mL | |
| 40 mM | 0.0245 mL | 0.1226 mL | 0.2453 mL | 0.6132 mL | |
| 50 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4906 mL | |
| 60 mM | 0.0164 mL | 0.0818 mL | 0.1635 mL | 0.4088 mL | |
| 80 mM | 0.0123 mL | 0.0613 mL | 0.1226 mL | 0.3066 mL | |
| 100 mM | 0.0098 mL | 0.0491 mL | 0.0981 mL | 0.2453 mL |