APL-1082
Based on 1 Customer Validation
APL-1082 is a drug-Linker conjugate that can be used for ADC synthesis. APL-1082 contains Exatecan (HY-13631) and Linker (HY-175929). APL-1082 reduces aggregation and hydrophobicity in Trastuzumab (HY-P9907) ADCs, enables production of high-DAR (10) ADCs with homogeneity and defined physicochemical properties. APL-1082 forms a Trastuzumab ADC with enhanced stability, showing greater DAR retention over time. APL-1082 can be used for the research of gastric cancer.
For research use only. We do not sell to patients.
- Purity : 95.58%
- CAS No.: 2921735-93-3
- Formula: C60H70FN11O16
- Molecular Weight:1220.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Drug-Linker Conjugates for ADC Isoforms
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Biological Activity
Description
In Vitro
APL-1082 conjugated Trastuzumab (DAR = 8) has higher hydrophilicity, shorter HIC retention time, and lower aggregation rate than Trastuzumab-deruxtecan (HY-138298A)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
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 mice (5 × 106 NCI-N87 cells was injected into the right hind flank for a xenograft model)[1]
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Dosage:1.25 mg/kg conjugated with Trastuzumab; 2.5 mg/kg conjugated with Trastuzumab
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Administration:tail vein injection; 4 doses on days 0, 4, 7, and 11
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Result:Inhibited tumor growth.
Chemical Information
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CAS No. 2921735-93-3
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Appearance Solid
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Molecular Weight 1220.26
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Formula C60H70FN11O16
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Color Light yellow to yellow
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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](NC(C)=O)CCC(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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Synonyms
Mc-exo-EVC-Exatecan
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (81.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8195 mL | 4.0975 mL | 8.1950 mL | 20.4874 mL |
| 5 mM | 0.1639 mL | 0.8195 mL | 1.6390 mL | 4.0975 mL | |
| 10 mM | 0.0819 mL | 0.4097 mL | 0.8195 mL | 2.0487 mL | |
| 15 mM | 0.0546 mL | 0.2732 mL | 0.5463 mL | 1.3658 mL | |
| 20 mM | 0.0410 mL | 0.2049 mL | 0.4097 mL | 1.0244 mL | |
| 25 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8195 mL | |
| 30 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6829 mL | |
| 40 mM | 0.0205 mL | 0.1024 mL | 0.2049 mL | 0.5122 mL | |
| 50 mM | 0.0164 mL | 0.0819 mL | 0.1639 mL | 0.4097 mL | |
| 60 mM | 0.0137 mL | 0.0683 mL | 0.1366 mL | 0.3415 mL | |
| 80 mM | 0.0102 mL | 0.0512 mL | 0.1024 mL | 0.2561 mL |