2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. APL-1082

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.

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APL-1082

APL-1082 Chemical Structure

CAS No. : 2921735-93-3

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Based on 1 publication(s) in Google Scholar

APL-1082 Related Antibodies

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Description

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[1].

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.

APL-1082 Related Antibodies
In Vivo

APL-1082 (1.25-2.5 mg/kg; tail vein injection; 4 doses on day 0, 4, 7, 11) conjugated Trastuzumab inhibits tumor growth in NOD.CB17 homozygous mice injected with NCI-N87 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD.CB17 homozygous mice (5 × 106 NCI-N87 cells was injected into the right hind flank for a xenograft model)[1]
Dosage: 1.25 mg/kg conjugated with Trastuzumab; 2.5 mg/kg conjugated with Trastuzumab
Administration: tail vein injection; 4 doses on days 0, 4, 7, and 11
Result: Inhibited tumor growth.
Molecular Weight

1220.26

Formula

C60H70FN11O16
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APL-1082 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APL-10822921735-93-3Mc-exo-EVC-ExatecanAPL1082APL 1082Drug-Linker Conjugates for ADCAJICAP first-generation conjugation technologytrastuzumabantibody-drug conjugatesratAJICAP second-generation conjugation technologygastric cancer xenograft modelsgastric cancerInhibitorinhibitorinhibit

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HY-175888
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