2. Cell Cycle/DNA Damage JAK/STAT Signaling Stem Cell/Wnt Immunology/Inflammation GPCR/G Protein
  3. Checkpoint Kinase (Chk) STAT CXCR CCR
  4. 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”.

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Zn-DPA-maytansinoid conjugate 1 Chemical Structure

Zn-DPA-maytansinoid conjugate 1 Chemical Structure

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Zn-DPA-maytansinoid conjugate 1 Related Antibodies

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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”[1].

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)[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.

Zn-DPA-maytansinoid conjugate 1 Related Antibodies

Cell Viability Assay[1]

Cell Line: Detroit 551, human pancreatic cancer MIA PaCa2 cells and triple-negative breast cancer HCC1806 cells
Concentration: 0-20 mM
Incubation Time: 72 hours
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).
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[1].

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

Animal Model: Nude mice bearing MIA PaCa-2, HCC1806 or sorafenib-resistant HCC xenograft tumors, respectively[1]
Dosage: 1 mg/kg, 2 mg/kg, 2.5 mg/kg
Administration: Intravenous injection; twice (day 1 and day 4) a week for 2 weeks; measured tumor twice weekly
Result: Resulted a lasting regression of tumor growth.
Animal Model: Male SD rats (8-week-old)[1]
Dosage: 1 mg/kg
Administration: Intravenous injection; once a week for 4 weeks (days 1, 8, 15, and 22); measured body weights daily
Result: Showed no effect on rats body weight.
Animal Model: Pharmacokinetic study in ICR mice (6-week-old) bearing HCC1806 tumors[1]
Dosage: 5 mg/kg (in 10% DMA/20% Cremophor EL/70% (5% dextrose))
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
Result: CL (mL/min/kg)=0.9; Vss (L/kg)=0.12; AUC (0-24 h) (ng/mL·h)=105599.
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.
Purity & Documentation
References
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Zn-DPA-maytansinoid conjugate 1 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:

Zn-DPA-maytansinoid conjugate 1Checkpoint Kinase (Chk)STATCXCRCCRCXC chemokine receptorsC-X-C motif chemokine receptorsCC chemokine receptorpancreatic cancertriple-negative breast cancersorafenib-resistant liver cancertumor microenvironmentinflamed hot tumormaytansinoid conjugateInhibitorinhibitorinhibit

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