| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Traditional Cytotoxic Agents
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|---|---|
| ln Vitro |
ADCs are made up of an antibody and an ADC cytotoxin that are joined together by an ADC link[1].
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| References | |
| Additional Infomation |
Antibody-drug conjugates are monoclonal antibodies conjugated to cytotoxic agents. They use antibodies that are specific to tumour cell-surface proteins and, thus, have tumour specificity and potency not achievable with traditional drugs. Design of effective antibody-drug conjugates for cancer therapy requires selection of an appropriate target, a monoclonal antibody against the target, potent cytotoxic effector molecules, and conjugation of the monoclonal antibody to cytotoxic agents. Substantial advances in all these aspects in the past decade have resulted in regulatory approval of ado-trastuzumab emtansine and brentuximab vedotin for clinical use. Several promising antibody-drug conjugates are now in late-phase clinical testing. Ongoing efforts are focused on identifying better targets, more effective cytotoxic payloads, and further improvements in antibody-drug linker technology. Improved understanding of the mechanistic basis of antibody-drug conjugate activity will enable design of rational combination therapies with other agents, including immunotherapy. [1]
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| Molecular Formula |
C72H79FN10O17
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|---|---|
| Molecular Weight |
1375.45
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| Exact Mass |
1374.56
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| CAS # |
2694856-51-2
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| PubChem CID |
162642643
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.43±0.1 g/cm3(Predicted)
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| LogP |
0.5
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
34
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| Heavy Atom Count |
100
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| Complexity |
3060
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| Defined Atom Stereocenter Count |
3
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| SMILES |
FC1=CC2=C3C(=C1C)CC[C@@H](C3=C1C(C3=CC4[C@](C(=O)OCC=4C(N3C1)=O)(CC)O)=N2)NC(COCNC(CNC([C@H](CC1C=CC=CC=1)NC(CNC(CNC(CCOCCOCCOCCOCCNC(CCC(N1C2C=CC=CC=2C#CC2C=CC=CC=2C1)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
UCUZJQMJKLKGGT-OHZCADGZSA-N
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| InChi Code |
InChI=1S/C72H79FN10O17/c1-3-72(94)52-34-58-68-50(40-83(58)70(92)51(52)41-100-71(72)93)67-54(20-19-49-44(2)53(73)35-55(81-68)66(49)67)79-64(89)42-99-43-78-62(87)37-77-69(91)56(33-45-11-5-4-6-12-45)80-63(88)38-76-61(86)36-75-60(85)23-25-95-27-29-97-31-32-98-30-28-96-26-24-74-59(84)21-22-65(90)82-39-48-15-8-7-13-46(48)17-18-47-14-9-10-16-57(47)82/h4-16,34-35,54,56,94H,3,19-33,36-43H2,1-2H3,(H,74,84)(H,75,85)(H,76,86)(H,77,91)(H,78,87)(H,79,89)(H,80,88)/t54-,56-,72-/m0/s1
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| Chemical Name |
4-(2-azatricyclo[10.4.0.04,9]hexadeca-1(16),4,6,8,12,14-hexaen-10-yn-2-yl)-N-[2-[2-[2-[2-[3-[[2-[[2-[[(2S)-1-[[2-[[2-[[(10S,23S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-5,9-dioxo-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaen-23-yl]amino]-2-oxoethoxy]methylamino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethyl]-4-oxobutanamide
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| Synonyms |
DBCO-PEG4-GGFG-Exatecan; DBCO-PEG4-GGFG-DX8951; 2694856-51-2; DBCO-PEG4-GGFG-Dxd; 7L3XY83XWU;
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 50 mg/mL (36.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.82 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 (1.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (1.82 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7270 mL | 3.6352 mL | 7.2703 mL | |
| 5 mM | 0.1454 mL | 0.7270 mL | 1.4541 mL | |
| 10 mM | 0.0727 mL | 0.3635 mL | 0.7270 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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