APL-1092
APL-1092 is an EEVC linker-payload conjugate composed of exatecan, a stabilizer that prevents premature payload release, and a cleavage substrate for cathepsin B. APL-1092 resists premature payload release mediated by human neutrophil elastase and carboxylesterase, maintains payload stability in mouse plasma, and retains cathepsin B-mediated cleavage activity in target cells. APL-1092 exhibits dose-dependent tumor growth inhibition in xenograft mice. APL-1092 can be used in gastric cancer-related research.
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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。
- CAS 番号: 2921735-91-1
- 分子式: C65H77FN12O19
- 分子量:1349.37
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
Drug-Linker Conjugates for ADC 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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.CB17 homozygous[1]
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Dosage:1.25 mg/kg; 2.5 mg/kg; 2.5 mg/kg; 10 mg/kg
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Administration:i.v.; once every 4 days; 11 days
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Result:Showed pronounced antitumor activity with a dose-dependent tumor-inhibitory effect.
Demonstrated substantial therapeutic efficacy at 2.5 mg/kg (AJICAP, DAR = 2, ADC (7)).
Showed superior tumor inhibitory effects compared to trastuzumab-deruxtecan when normalized to incorporated payload amount (AJICAP, DAR = 2, ADC (7)).
Showed significant tumor growth inhibitory effects at both 1.25 mg/kg and 2.5 mg/kg (interchain-break, DAR = 8, ADC (9)).
化学情報
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CAS 番号 2921735-91-1
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性状 Solid
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分子量 1349.37
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分子式 C65H77FN12O19
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SMILES
O=C(C=CC1=O)N1CCCCCNC(C(C2=CC=C(C=C2)NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC([C@H](CCC(O)=O)NC([C@@H](NC(C)=O)CCC(O)=O)=O)=O)=O)=O)OC(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C84)=O)=O
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別名
Mal-Exo-EEVC-Exatecan
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (74.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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
参考文献
[1]. Watanabe T, et al. Exo-Cleavable Linkers: Enhanced Stability and Therapeutic Efficacy in Antibody-Drug Conjugates. Journal of medicinal chemistry. 2024 Oct 24;67(20):18124-18138. [Content Brief]
[2]. Watanabe T, et al. Homogeneous Dual-Payload Antibody-Drug Conjugates Produced by Combined Distinct Conjugation Strategies. ACS medicinal chemistry letters. 2025 Jul 10;16(7):1334-1339. [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 (protect from light, stored under nitrogen). 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 | 0.7411 mL | 3.7054 mL | 7.4109 mL | 18.5272 mL |
| 5 mM | 0.1482 mL | 0.7411 mL | 1.4822 mL | 3.7054 mL | |
| 10 mM | 0.0741 mL | 0.3705 mL | 0.7411 mL | 1.8527 mL | |
| 15 mM | 0.0494 mL | 0.2470 mL | 0.4941 mL | 1.2351 mL | |
| 20 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9264 mL | |
| 25 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7411 mL | |
| 30 mM | 0.0247 mL | 0.1235 mL | 0.2470 mL | 0.6176 mL | |
| 40 mM | 0.0185 mL | 0.0926 mL | 0.1853 mL | 0.4632 mL | |
| 50 mM | 0.0148 mL | 0.0741 mL | 0.1482 mL | 0.3705 mL | |
| 60 mM | 0.0124 mL | 0.0618 mL | 0.1235 mL | 0.3088 mL |
APL-1092 関連分類
HY-169324 関連分類
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