Larotinib
Based on 1 Customer Validation
Larotinib (Z650) is an orally active ErbB family receptor tyrosine kinase inhibitor with EGFR as its primary target and an IC50 of 0.6 nM. Larotinib inhibits wild-type and mutant EGFR as well as HER2/HER4 (IC50 of 253 and 84 nM). Larotinib inhibits RIPK2, IRAK1, BTK, and BLK, with target IC50 values of 26.6, 167, 196, and 102 nM, respectively. Larotinib is primarily metabolized by CYP3A4 in vitro. Larotinib can be used for research on advanced solid tumors.
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 : 99.50%
- CAS 番号: 1438072-11-7
- 分子式: C24H26ClFN4O4
- 分子量:488.94
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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
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
製品説明
IC50 & Target
[1]|
EGFRL861Q 0.423 nM (IC50) |
EGFRL858R 0.563 nM (IC50) |
EGFR (WT) 0.611 nM (IC50) |
RIPK2 26.6 nM (IC50) |
EGFRT790M 45.2 nM (IC50) |
HER4 84 nM (IC50) |
BLK 102 nM (IC50) |
IRAK1 167 nM (IC50) |
BTK 196 nM (IC50) |
HER2 253 nM (IC50) |
体外実験
Larotinib (100 μM) inhibits PRDX1 Tyr194 phosphorylation in HRECs at a minimum effective dose of 100 μM[2].
Larotinib (100 μM) shifts PRDX1 from high-
molecular-weight (HMW) dimers toward low-molecular-weight (LMW) monomers in KIF11-knockdown HRECs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Larotinib produces dose-dependent tumor growth inhibition in tumor-bearing mice, exceeding 60% inhibition at 18 mg/kg[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 1438072-11-7
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性状 Solid
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分子量 488.94
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分子式 C24H26ClFN4O4
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Color White to off-white
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SMILES
COC(C(OCCCN1C[C@]2([H])[C@](OCCO2)([H])C1)=C3)=CC4=C3C(NC5=CC(Cl)=C(C=C5)F)=NC=N4
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別名
Z650
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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
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (255.66 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 (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Liu J, et al. Phase I Trial to Evaluate the Tolerance, Pharmacokinetics and Efficacy of the Broad-Spectrum ErbB Family Inhibitor Larotinib Mesylate in Patients With Advanced Solid Tumors. Front Pharmacol. 2021 Feb 18;12:636324. [Content Brief]
[2]. Yang M, et al. KIF11 prevents retinal endothelial ferroptosis in familial exudative vitreoretinopathy by inhibiting phosphorylation-driven PRDX1 phase separation. Nature communications. 2026 Mar 24;17(1):4360. [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. 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 | 2.0452 mL | 10.2262 mL | 20.4524 mL | 51.1310 mL |
| 5 mM | 0.4090 mL | 2.0452 mL | 4.0905 mL | 10.2262 mL | |
| 10 mM | 0.2045 mL | 1.0226 mL | 2.0452 mL | 5.1131 mL | |
| 15 mM | 0.1363 mL | 0.6817 mL | 1.3635 mL | 3.4087 mL | |
| 20 mM | 0.1023 mL | 0.5113 mL | 1.0226 mL | 2.5566 mL | |
| 25 mM | 0.0818 mL | 0.4090 mL | 0.8181 mL | 2.0452 mL | |
| 30 mM | 0.0682 mL | 0.3409 mL | 0.6817 mL | 1.7044 mL | |
| 40 mM | 0.0511 mL | 0.2557 mL | 0.5113 mL | 1.2783 mL | |
| 50 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0226 mL | |
| 60 mM | 0.0341 mL | 0.1704 mL | 0.3409 mL | 0.8522 mL | |
| 80 mM | 0.0256 mL | 0.1278 mL | 0.2557 mL | 0.6391 mL | |
| 100 mM | 0.0205 mL | 0.1023 mL | 0.2045 mL | 0.5113 mL |
Larotinib 関連分類
HY-153110 関連分類
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Keywords
- Larotinib
- 1438072-11-7
- Z650
- Z 650
- Z-650
- EGFR
- IRAK
- Btk
- RIP kinase
- Epidermal growth factor receptor
- ErbB-1
- HER1
- Interleukin-1 receptor associated kinase
- IL-1R associated kinase
- Bruton tyrosine kinase
- Receptor-interacting protein kinases
- RIPK
- BLK
- BTK
- ErbB family receptor tyrosine kinase
- HER2
- HER4
- IRAK1
- PRDX1
- RIPK2
- advanced solid tumors
- Inhibitor
- inhibitor
- inhibit