Mobocertinib succinate
Based on 12 publication(s) in Google Scholar
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.
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 : 99.83%
- CAS 番号: 2389149-74-8
- 分子式: C36H45N7O8
- 分子量:703.78
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
MedChemExpress（MCE）の使用を引用している文献 Mobocertinib succinate
More- Cancer Res. 2025 Nov 6. [Abstract]
- Acta Pharm Sin B. 2023 Jun;13(6):2613-2627. [Abstract]
- Clin Cancer Res. 2025 Jun 4:OF1-OF17. [Abstract]
- Cells. 2021 Dec 17;10(12):3561. [Abstract]
- Lung Cancer. 2025 Apr:202:108479. [Abstract]
- Lung Cancer. 2023 Jul:181:107250. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- JTO Clin Res Rep. 2023 Nov 27;5(1):100614. [Abstract]
- JTO Clin Res Rep. 2023 Jan 24;4(3):100462. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 16:780:152460. [Abstract]
- Biomed Chromatogr. 2025 Feb;39(2):e6063. [Abstract]
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
EGFR exon 20 insertion |
HER2 |
EGFR (WT) |
体外実験
Mobocertinib succinate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM[1].
Mobocertinib succinate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))[1].
Mobocertinib succinate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib succinate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib succinate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:LU0387 (NPH) cells
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Concentration:1.5 nM-10 μM
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Incubation Time:7 days
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Result:Showed good inhibition activity for LU0387 (NPH) cells with IC50 of 21 nM.
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Cell Line:A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
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Concentration:
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Incubation Time:2 h
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Result:Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC50s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC50 of 35 nM).
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Cell Line:CUTO14 (ASV) cells
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Concentration:0.1 nM-1 μM
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Incubation Time:6 h
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Result:Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.
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Cell Line:HCC827 (D), HCC4011 (L), H1975 (LT) cells
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Concentration:0.3 nM-1 μM
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Incubation Time:6 h
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Result:Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.
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Cell Line:H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells
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Concentration:0.01, 0.1 and 1 μM
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Incubation Time:6 h
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Result:Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model)[1].
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Dosage:3, 10, 30 mg/kg
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Administration:Oral; once daily for 20 days.
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Result:Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2389149-74-8
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性状 Solid
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分子量 703.78
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分子式 C36H45N7O8
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Color White to yellow
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SMILES
O=C(C1=CN=C(NC2=CC(NC(C=C)=O)=C(N(CCN(C)C)C)C=C2OC)N=C1C3=CN(C)C4=C3C=CC=C4)OC(C)C.O=C(O)CCC(O)=O
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別名
TAK-788 succinate; AP32788 succinate
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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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Res
Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]2025 Nov 6. PMID: 41196054 -
Acta Pharm Sin B
Antitumor activity of aumolertinib, a third-generation EGFR tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon EGFR mutations. [Abstract]2023 Jun;13(6):2613-2627. PMID: 37425047 -
Clin Cancer Res
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]2025 Jun 4:OF1-OF17. PMID: 40465424 -
Cells
EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios. [Abstract]2021 Dec 17;10(12):3561. PMID: 34944068 -
Lung Cancer
Efficacy of EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer with EGFR exon 19 insertions: clinical-genomic, preclinical analysis through LC-SCRUM-Asia (multi-institutional genomic screening registry). [Abstract]2025 Apr:202:108479. PMID: 40088581 -
Lung Cancer
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors. [Abstract]2023 Jul:181:107250. PMID: 37196448 -
Toxicology
Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]2024 May 15:505:153830. PMID: 38754619 -
Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
JTO Clin Res Rep
The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors. [Abstract]2023 Nov 27;5(1):100614. PMID: 38229766 -
JTO Clin Res Rep
The EGFR C797S Mutation Confers Resistance to a Novel EGFR Inhibitor CLN-081 to EGFR Exon 20 Insertion Mutations. [Abstract]2023 Jan 24;4(3):100462. PMID: 36915628 -
Biochem Biophys Res Commun
Electrophysiological consequences of acute mobocertinib exposure in isolated rat and guinea-pig hearts and transfected cell lines. [Abstract]2025 Sep 16:780:152460. PMID: 40818285 -
Biomed Chromatogr
A Simple and Sensitive LC-MS/MS Method for the Determination of Mobocertinib and Its Metabolite Desmethyl-Mobocertinib in Human Plasma and Its Application to Clinical Pharmacokinetic Study. [Abstract]2025 Feb;39(2):e6063. PMID: 39748454
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (177.61 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 (sealed storage, away from moisture). 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). 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)
体内:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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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)
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 (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gonzalvez F, et al. Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687. [Content Brief]
[2]. an H, et al. Targeting HER2 Exon 20 Insertion-Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib. Cancer Res. 2021 Oct 15;81(20):5311-5324. [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). 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 | 1.4209 mL | 7.1045 mL | 14.2090 mL | 35.5225 mL |
| 5 mM | 0.2842 mL | 1.4209 mL | 2.8418 mL | 7.1045 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4209 mL | 3.5522 mL | |
| 15 mM | 0.0947 mL | 0.4736 mL | 0.9473 mL | 2.3682 mL | |
| 20 mM | 0.0710 mL | 0.3552 mL | 0.7104 mL | 1.7761 mL | |
| 25 mM | 0.0568 mL | 0.2842 mL | 0.5684 mL | 1.4209 mL | |
| 30 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 1.1841 mL | |
| 40 mM | 0.0355 mL | 0.1776 mL | 0.3552 mL | 0.8881 mL | |
| 50 mM | 0.0284 mL | 0.1421 mL | 0.2842 mL | 0.7104 mL | |
| 60 mM | 0.0237 mL | 0.1184 mL | 0.2368 mL | 0.5920 mL | |
| 80 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.4440 mL | |
| 100 mM | 0.0142 mL | 0.0710 mL | 0.1421 mL | 0.3552 mL |
Mobocertinib succinate 関連分類
HY-135815A 関連分類
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