ABN401
Based on 1 Customer Validation
ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC50 of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC50 of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 98.82%
- CAS 番号: 2242563-15-9
- 分子式: C29H34N12O
- 分子量:566.66
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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生物活性
IC50: 10 nM (c-MET)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EBC-1 | IC50 |
2.22 nM
Compound: 73; ABN401
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Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| Hs746T | IC50 |
2 nM
Compound: 73; ABN401
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Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth
Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| MKN-45 | IC50 |
3.18 nM
Compound: 73; ABN401
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Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| SNU-5 | IC50 |
4.34 nM
Compound: 73; ABN401
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Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth
Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
ABN401 (0.1-10 μM; 72 h) inhibits c-MET activation and downstream signaling pathway, and induces apoptosis signaling pathway activation in MET addicted cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU5, SNU638, Hs746T, EBC-1 and H1993 cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:72 h
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Result:Inhibited the phosphorylation levels of MET, AKT and ERK1/2.
Increased the levels of cleaved caspase-3 and cleaved PARP-1.
ABN401 (3-30 mg/kg; oral administration; once a day for 3 weeks) shows antitumor activity in a xenograft model derived from patients with non-small cell lung cancer in mice, and the combination with Erlotinib (HY-50896) has better effect[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SNU5, EBC-1 and SNU638 treated BALB/c-nude mice[1]
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Dosage:3, 10 and 30 mg/kg
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Administration:Oral administration (p.o.); Five consecutive days a week for three weeks
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Result:Significantly inhibited tumor growth in a dose-dependent manner.
Significantly suppressed SNU-5 tumor growth with a TGI index of 24.47% and 89.49% at doses of 3 and 30 mg/kg, respectively.
Inhibited EBC-1 tumor growth with a TGI index of 51.26% and 77.85% at doses of 10 and 30 mg/kg, respectively.
Suppressed SNU638 tumor growth with a TGI index of 65.31% and 78.68% at doses of 10 and 30 mg/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2242563-15-9
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性状 Solid
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分子量 566.66
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分子式 C29H34N12O
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Color Off-white to light yellow
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SMILES
CN1N=CC(C2=CN=C3C(N(CC4CN(C5=NC=C(C6=CC=C(CN7CCN(C)CC7)C=C6)C=N5)CCO4)N=N3)=N2)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 10 mg/mL (17.65 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.76 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.76 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
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- Français - FR (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kim J, et al. Therapeutic Efficacy of ABN401, a Highly Potent and Selective MET Inhibitor, Based on Diagnostic Biomarker Test in MET-Addicted Cancer. Cancers (Basel). 2020;12(6):1575. Published 2020 Jun 15. [Content Brief]
[2]. Kim NA, et al. New Preclinical Development of a c-Met Inhibitor and Its Combined Anti-Tumor Effect in c-Met-Amplified NSCLC. Pharmaceutics. 2020 Feb 3;12(2):121. [Content Brief]
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 (sealed storage, away from moisture and light). 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 | 1.7647 mL | 8.8236 mL | 17.6473 mL | 44.1182 mL |
| 5 mM | 0.3529 mL | 1.7647 mL | 3.5295 mL | 8.8236 mL | |
| 10 mM | 0.1765 mL | 0.8824 mL | 1.7647 mL | 4.4118 mL | |
| 15 mM | 0.1176 mL | 0.5882 mL | 1.1765 mL | 2.9412 mL |
ABN401 関連分類
HY-147040 関連分類
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