Zn-DPA-maytansinoid conjugate 1
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
For research use only. We do not sell to patients.
- CAS No.: 3034629-04-1
- Formula: C115H145ClN18O31S2Zn2
- Molecular Weight:2505.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Zn-DPA-maytansinoid conjugate 1 (compound 40a) (0-20 mM; 72 h) inhibits the growth of human pancreatic cancer MIA PaCa2 cells and triple-negative breast cancer HCC1806 cells and displays no effect on normal fibroblast (Detroit 551)[1].
Zn-DPA-maytansinoid conjugate 1 increases CD8+ T cell infiltration significantly in the tumor mass that sensitized tumors from the intrinsic immune-suppressive TME[1].
Zn-DPA-maytansinoid conjugate 1 induces tumor inflammation-related mRNA expression such as STAT1, CXCL10, CCL5, and CCL2[1].
Zn-DPA-maytansinoid conjugate 1 leads to rejuvenation of TME with enhancement in T cell, macrophage, NK cell, chemokine, and cytokine functions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Detroit 551, human pancreatic cancer MIA PaCa2 cells and triple-negative breast cancer HCC1806 cells
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Concentration:0-20 mM
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Incubation Time:72 hours
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Result:Inhibited cancer cells with IC50s of 676 nM (MIA PaCa2) and 39 nM (HCC1806), respectively.
Showed low cytotoxicity against Detroit 551 cells (IC50>20 mM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice bearing MIA PaCa-2, HCC1806 or sorafenib-resistant HCC xenograft tumors, respectively[1]
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Dosage:1 mg/kg, 2 mg/kg, 2.5 mg/kg
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Administration:Intravenous injection; twice (day 1 and day 4) a week for 2 weeks; measured tumor twice weekly
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Result:Resulted a lasting regression of tumor growth.
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Animal Model:Male SD rats (8-week-old)[1]
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Dosage:1 mg/kg
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Administration:Intravenous injection; once a week for 4 weeks (days 1, 8, 15, and 22); measured body weights daily
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Result:Showed no effect on rats body weight.
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Animal Model:Pharmacokinetic study in ICR mice (6-week-old) bearing HCC1806 tumors[1]
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Dosage:5 mg/kg (in 10% DMA/20% Cremophor EL/70% (5% dextrose))
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Administration:Intravenous injection; single dose; collected blood samples at 0.003, 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h and collected tumor samples at 0.5, 2, 6, 24, 72, and 168 h
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Result:CL (mL/min/kg)=0.9; Vss (L/kg)=0.12; AUC (0-24 h) (ng/mL·h)=105599.
Chemical Information
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CAS No. 3034629-04-1
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Molecular Weight 2505.83
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Formula C115H145ClN18O31S2Zn2
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SMILES
[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.C[C@H](C(O[C@@H](CC(N1C)=O)[C@](O2)(C)C2[C@@H](C)[C@@H]3OC(N[C@](O)([C@H](/C=C\C=C(CC4=CC(OC)=C(C1=C4)Cl)/C)OC)C3)=O)=O)N(C(CCSSCCC(NCC5=CC=C(CNC(COCCOCCOCC(N(CCCCOC6=CC(C[N]78CC9=CC=CC=[N]9[Zn+2]7[N](C(NC(CCCCC)=O)=CC=C%10)=C%10C8)=CC(C[N]%11%12CC%13=CC=CC=[N]%13[Zn+2]%11[N](C(NC(CCCCC)=O)=CC=C%14)=C%14C%12)=C6)CC%15=CC=C(C=C%15)C%16=CC=CC=C%16)=O)=O)C=C5)=O)=O)C
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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