| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Maytansinoids
Microtubules (tubulin). As a maytansinoid, it binds to tubulin at the maytansine-binding site (near the vinca domain), inhibiting microtubule polymerization and causing mitotic arrest and cell death. |
|---|---|
| ln Vitro |
The maytansinoid payload is a highly potent cytotoxin, with IC50 values in the picomolar to low nanomolar range (0.1-10 nM) against cancer cell lines. As a payload, its activity is dependent on delivery by the ADC. N-Me-L-Ala-maytansinol is a hydrophobic, cell-permeable payload. Preclinical studies demonstrate its utility as a cytotoxic warhead for ADCs.
|
| ln Vivo |
In vivo, ADCs containing this payload are designed to target tumor cells, delivering the potent cytotoxin selectively, improving the therapeutic index. The ADC approach reduces systemic toxicity by targeting the payload specifically to tumor cells expressing the target antigen.
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| Enzyme Assay |
Not applicable for the payload itself. Tubulin polymerization assays can be used to confirm the mechanism of action of the released maytansinoid: purified tubulin is incubated with the maytansinoid (0.01-100 nM) and polymerization is monitored by turbidity at 340 nm.
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| Cell Assay |
Cell viability assay: Cancer cells expressing the target antigen are seeded in 96-well plates and treated with the ADC containing N-Me-L-Ala-maytansinol (0.001-1000 nM) or the free payload for 72-96 hours. Cell viability is measured using MTT or CellTiter-Glo. Target-dependent killing confirms ADC specificity.
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| Animal Protocol |
Mouse xenograft models: ADCs containing the payload are administered to tumor-bearing mice (intravenous, 1-10 mg/kg, single or multiple doses). Tumor growth inhibition is measured, and pharmacodynamic markers (mitotic arrest, apoptosis) are assessed.
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| ADME/Pharmacokinetics |
The pharmacokinetics of ADCs containing this payload are determined by the antibody component, with a long half-life and slow clearance characteristic of monoclonal antibodies. The payload itself is not administered as a free drug.
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| Toxicity/Toxicokinetics |
As a maytansinoid, the payload can cause myelosuppression, gastrointestinal effects, and neuropathy. The ADC approach aims to reduce systemic toxicity.
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| References | |
| Additional Infomation |
This is a research reagent used in ADC development. Molecular weight: 650.16, formula: C32H44ClN3O9. CAS number: 77668-69-0. It is a hydrophobic, cell-permeable maytansinoid payload used as a cytotoxic warhead for constructing ADCs.
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| Molecular Formula |
C32H44CLN3O9
|
|---|---|
| Molecular Weight |
650.159468650818
|
| Exact Mass |
649.28
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| Elemental Analysis |
C, 59.12 H, 6.82 Cl, 5.45 N, 6.46 O, 22.15
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| CAS # |
77668-69-0
|
| PubChem CID |
90254243
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| Appearance |
White to off-white solid powder
|
| LogP |
2.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
45
|
| Complexity |
1170
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C/C=C(/CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@@H]([C@]4([C@H]1O4)C)OC(=O)[C@H](C)NC)C)\C)OC)(NC(=O)O2)O
|
| InChi Key |
ANHBJISROJTYCJ-MSKZWLSNSA-N
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| InChi Code |
InChI=1S/C32H44ClN3O9/c1-17-10-9-11-24(42-8)32(40)16-23(43-30(39)35-32)18(2)28-31(4,45-28)25(44-29(38)19(3)34-5)15-26(37)36(6)21-13-20(12-17)14-22(41-7)27(21)33/h9-11,13-14,18-19,23-25,28,34,40H,12,15-16H2,1-8H3,(H,35,39)/b11-9+,17-10+/t18-,19+,23+,24-,25+,28+,31+,32+/m1/s1
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| Chemical Name |
(14S,16S,32S,33S,2R,4S,10E,12E,14R)-86-chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl methyl-L-alaninate
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| Synonyms |
Maytansinol-Ala;
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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 |
| 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 (~153.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5381 mL | 7.6904 mL | 15.3808 mL | |
| 5 mM | 0.3076 mL | 1.5381 mL | 3.0762 mL | |
| 10 mM | 0.1538 mL | 0.7690 mL | 1.5381 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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