| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Zn-DPA-maytansinoid conjugate 1 (compound 40a) (0–20 mM; 72 h) inhibits triple-negative breast cancer HCC1806 cells and human pancreatic cancer MIA PaCa2 cells while having no effect on normal fibroblast (Detroit 551)[1].
Zn-DPA-maytansinoid conjugate 1 sensitizes tumors to the intrinsic immune-suppressive TME by greatly increasing CD8+ T cell infiltration in the tumor mass[1]. Zn-DPA-maytansinoid conjugate 1 stimulates the expression of mRNAs linked to tumor inflammation, including STAT1, CXCL10, CCL5, and CCL2[1]. Zn-DPA-maytansinoid conjugate 1 stimulates T cell, macrophage, NK cell, chemokine, and cytokine functions, resulting in TME rejuvenation[1]. |
|---|---|
| ln Vivo |
Zn-DPA-maytansinoid conjugate 1 (compound 40a) (1-2.5 mg/kg; i.v.; twice weekly for 2 weeks) exhibited anti-tumor activities against sorafenib-resistant HCC, anti-pancreatic cancer, and anti-triple-negative breast cancer[1].
|
| Cell Assay |
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). |
| Animal Protocol |
Nude mice bearing MIA PaCa-2, HCC1806 or sorafenib-resistant HCC xenograft tumors, respectively[1]
1 mg/kg, 2 mg/kg, 2.5 mg/kg Intravenous injection; twice (day 1 and day 4) a week for 2 weeks; measured tumor twice weekly |
| References |
| Molecular Formula |
C115H145CLN18O31S2ZN2
|
|---|---|
| Molecular Weight |
2505.83
|
| Synonyms |
Zn-DPA-maytansinoid conjugate 1
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3991 mL | 1.9953 mL | 3.9907 mL | |
| 5 mM | 0.0798 mL | 0.3991 mL | 0.7981 mL | |
| 10 mM | 0.0399 mL | 0.1995 mL | 0.3991 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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