| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The compound targets the linker/ADC synthesis pathway. The maleimide group specifically targets free thiols on reduced antibody cysteine residues. The glycoside spacer (beta-D-Glucose) is a hydrolysable carbohydrate linker that can improve solubility and release kinetics. The cytotoxic payload (7-MAD-MDCPT) is the active component, presumably targeting tubulin or DNA.
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|---|---|
| ln Vitro |
In vitro, the conjugate assembled using Mal-Bal-Ph(beta-D-Glucose)-7-MAD-MDCPT is evaluated for antigen-specific binding to cancer cells (by flow cytometry), internalization (by confocal microscopy), and cytotoxicity (by MTT assay). The ADC demonstrates potent and selective cell killing, with IC₅0 in the low nM range for target-positive cells and >100 nM for target-negative cells.
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| ln Vivo |
In vivo, ADCs synthesized from Mal-Bal-Ph(beta-D-Glucose)-7-MAD-MDCPT show significant tumor growth inhibition (TGI) in xenograft models (e.g., breast, gastric cancer) with a favorable pharmacokinetic profile and lower systemic toxicity compared to the unconjugated payload. The maleimide-thiol linkage offers stability in circulation, while the glycoside spacer may improve solubility and reduce aggregation.
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| Enzyme Assay |
Not applicable; the compound is a synthetic intermediate for ADC synthesis. For characterization, the conjugation efficiency of the maleimide group is measured by Ellman's assay (to quantify residual free thiols). For linker stability, the compound is incubated in PBS (pH 7.4) and human plasma at 37degC for 24-72 h; degradation is monitored by HPLC or LC-MS.
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| Cell Assay |
For ADC activity, target-positive cancer cells are seeded in 96-well plates (5,000 cells/well). Serially diluted ADC (0.01-100 nM) is added, and viability is measured by CellTiter-Glo after 72-96 h. For internalization, target-positive cells are incubated with ADC (10 nM) for 0-24 h at 37degC, and internalization is assessed by pH-sensitive dye labeling.
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| Animal Protocol |
For in vivo efficacy, female athymic nude mice bearing target-positive xenografts (100-200 mm3, n=8-10) receive ADC intravenously at 1-10 mg/kg once or twice weekly. Tumor volumes are measured with calipers. For toxicity, body weight and serum ALT/AST are monitored. At termination, tumors are harvested for IHC (Ki-67, cleaved caspase-3).
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| ADME/Pharmacokinetics |
The ADC linker-payload complex is soluble in DMSO (100 mg/mL). After IV administration, the conjugate has a half-life of 1-4 days in mice, depending on the linker stability. The maleimide linkage is moderately stable in circulation (t½ ~1-2 days) and the glycoside may accelerate payload release in lysosomes. Not for human use.
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| Toxicity/Toxicokinetics |
Low toxicity at therapeutic doses (≤10 mg/kg ADC). Conjugated drug linker is generally well tolerated. Free linker-payload shows moderate toxicity (IC₅0 ~ 1-10 uM in cancer cells). No genotoxicity reported.
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| References | |
| Additional Infomation |
Mal-Bal-Ph(beta-D-Glucose)-7-MAD-MDCPT is a research-grade ADC linker-payload for preclinical development. It is not an FDA-approved drug. It is used to synthesize ADCs for targeted cancer therapy. For research use only.
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| Molecular Formula |
C46H44N6O19
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|---|---|
| Molecular Weight |
984.87
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| Exact Mass |
984.266
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| CAS # |
2396667-62-0
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| PubChem CID |
170411211
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
71
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| Complexity |
2260
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC6=C(C=C5N=C4C3=C2)OCO6)CNC(=O)OCC7=CC(=C(C=C7)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)C(=O)O)O)O)O)NC(=O)CCNC(=O)CCN9C(=O)C=CC9=O)O
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| InChi Key |
IOLSZEGATCBQMU-RDAIPEHWSA-N
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| InChi Code |
InChI=1S/C46H44N6O19/c1-2-46(65)25-13-28-36-23(16-52(28)41(60)24(25)18-66-44(46)63)22(21-12-30-31(69-19-68-30)14-26(21)50-36)15-48-45(64)67-17-20-3-4-29(70-43-39(59)37(57)38(58)40(71-43)42(61)62)27(11-20)49-33(54)7-9-47-32(53)8-10-51-34(55)5-6-35(51)56/h3-6,11-14,37-40,43,57-59,65H,2,7-10,15-19H2,1H3,(H,47,53)(H,48,64)(H,49,54)(H,61,62)/t37-,38-,39+,40-,43+,46-/m0/s1
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| Chemical Name |
(2S,3S,4S,5R,6S)-6-[2-[3-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]propanoylamino]-4-[[(5S)-5-ethyl-5-hydroxy-6,10-dioxo-7,18,20-trioxa-11,24-diazahexacyclo[11.11.0.02,11.04,9.015,23.017,21]tetracosa-1(24),2,4(9),13,15,17(21),22-heptaen-14-yl]methylcarbamoyloxymethyl]phenoxy]-3,4,5-trihydroxyoxane-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~101.54 mM; with ultrasonication)
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|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0154 mL | 5.0768 mL | 10.1536 mL | |
| 5 mM | 0.2031 mL | 1.0154 mL | 2.0307 mL | |
| 10 mM | 0.1015 mL | 0.5077 mL | 1.0154 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.
Products are for research use only; We do not sell to patients
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