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Cat. No.: HY-189369

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Antiproliferative agent-81

Antiproliferative agent-81 is a Homocamptothecin-derived ADC payload (ADC Payload) featuring an expanded seven-membered β-hydroxylactone ring. Antiproliferative agent-81 exhibits antiproliferative activity against multiple cancer cell lines with varying HER2 expression levels. Antiproliferative agent-81 is applicable to ADC synthesis-related research.

For research use only. We do not sell to patients.

Formula: C₂₇H₂₉FN₂O₆
Molecular Weight:496.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Antiproliferative agent-81 Chemical Structure

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Use of MCE Products

One-Stop Platform：From Independent R&D to Pilot-Scale Production

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
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Biological Activity

Description

All ADC Payloads Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	0.3901 nM	Antiproliferative activity against human MDA-MB-231 breast carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay. Antiproliferative activity against human MDA-MB-231 breast carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay.	42720475
JIMT-1	IC50	4.374 nM	Antiproliferative activity against human JIMT-1 breast carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay. Antiproliferative activity against human JIMT-1 breast carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay.	42720475
NCI-N87	IC50	1.118 nM	Antiproliferative activity against human NCI-N87 gastric carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay. Antiproliferative activity against human NCI-N87 gastric carcinoma cells assessed as reduction in cell viability by proliferation inhibition assay.	42720475

In Vitro

Anti-cancer

Antiproliferative agent-81 (Serially diluted concentrations) exhibits superior intrinsic cytotoxicity against MDA-MB-231 (IC₅₀ = 0.3901 nM), JIMT-1 (IC₅₀ = 4.374 nM), and NCI-N87 (IC₅₀ = 1.118 nM) cancer cell lines compared to conventional six-membered α-hydroxylactone analogs^[1].

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

Related Protocols :

Chemical Information

Molecular Weight 496.53
Formula C₂₇H₂₉FN₂O₆
SMILES

OCCCCC1=C2C(C(N3C2)=CC([C@@](O)(CC)[C@H](OC)C(OC4)=O)=C4C3=O)=NC5=CC(F)=C(C)C=C51
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Xie J, et al. Homocamptothecin Payloads with Enhanced Potency for Antibody-Drug Conjugates. Journal of medicinal chemistry. 2026 Sep 10;69(17):20213-20229.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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