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Zn-DPA-maytansinoid conjugate 1

Zn-DPA-maytansinoid conjugate 1

Zn-DPA-maytansinoid conjugate 1

Catalog No.: PC0176

Size: 50 mg, 100mg, 250mg


Description

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”.

Molecular Weight 2505.83
Formula C115H145ClN18O31S2Zn2
SMILES [O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.C[C@@H](N(C)C(CCSSCCC(NCC1=CC=C(C=C1)CNC(COCCOCCOCC(N(CC2=CC=C(C3=CC=CC=C3)C=C2)CCCCOC4=CC(C[N]5(CC6=CC=CC=[N]6[Zn+2]75)CC8=[N]7C(NC(CCCCC)=O)=CC=C8)=CC(C[N]9(CC%10=CC=CC=[N]%10[Zn+2]%119)CC%12=[N]%11C(NC(CCCCC)=O)=CC=C%12)=C4)=O)=O)=O)=O)C(O[C@H]([C@](C%13[C@H]([C@H](OC(N%14)=O)C[C@@]%14(O)[C@@H](OC)/C=C\C=C(C)\CC%15=CC(OC)=C(Cl)C%16=C%15)C)(O%13)C)CC(N%16C)=O)=O
Shipping Room temperature in continental US; may vary elsewhere.
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
In Vitro 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).
Zn-DPA-maytansinoid conjugate 1 increases CD8+ T cell infiltration significantly in the tumor mass that sensitized tumors from the intrinsic immune-suppressive TME.
Zn-DPA-maytansinoid conjugate 1 induces tumor inflammation-related mRNA expression such as STAT1, CXCL10, CCL5, and CCL2.
Zn-DPA-maytansinoid conjugate 1 leads to rejuvenation of TME with enhancement in T cell, macrophage, NK cell, chemokine, and cytokine functions.
In Vivo Zn-DPA-maytansinoid conjugate 1 (compound 40a) (1-2.5 mg/kg; i.v.; twice a week for 2 weeks) effectively shrank the growth of many solid tumors, exerts antipancreatic cancer, anti-triple-negative breast cancer and anti-sorafenib-resistant HCC tumor activities.
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