| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg |
| Targets |
ADC linker
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|---|---|
| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1].
|
| References |
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
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| Additional Infomation |
Antibody-drug conjugates (ADCs) are among the fastest-growing drugs in the field of cancer treatment. After half a century of research, the approval of brentuximab (2011) and trastuzumab (2013) paved the way for ongoing clinical trials that are evaluating more than 60 other ADC candidates. Limited success of first-generation ADCs (developed in the early 21st century) has prompted the development of strategies to bring second-generation ADCs to market. Second-generation ADCs have higher levels of cytotoxic drug conjugation, lower levels of naked antibody, and more stable drug-antibody linkers. In addition, experience accumulated over the past decade is being used to develop third-generation ADCs. In this review, we will discuss how to select the best target antigen and appropriate cytotoxic drug; optimize the design of linkers; discover bioorthogonal coupling chemistry; and toxicity issues. The focus of antibody-drug conjugate (ADC) research is on selecting and modifying antibodies for site-specific drug conjugation, which will lead to higher uniformity and stability, as well as exploring new coupling chemistry and mechanisms of action. [1]
|
| Molecular Formula |
C₃₇H₅₀F₅N₅O₁₀
|
|---|---|
| Molecular Weight |
819.81
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| Exact Mass |
819.347
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| Elemental Analysis |
C, 54.21; H, 6.15; F, 11.59; N, 8.54; O, 19.52
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| CAS # |
2353409-45-5
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| PubChem CID |
138373725
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.3
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
57
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| Complexity |
1350
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CCCNC(=O)N)C(=O)OC1=C(C(=C(C(=C1F)F)F)F)F)NC(=O)CCOCCOCCOCCNC(=O)OCC2[C@H]3[C@@H]2CCC#CCC3
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| InChi Key |
ODFSIYMVJDIAIS-COWKONOXSA-N
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| InChi Code |
InChI=1S/C37H50F5N5O10/c1-21(2)32(34(49)46-25(10-7-12-44-36(43)51)35(50)57-33-30(41)28(39)27(38)29(40)31(33)42)47-26(48)11-14-53-16-18-55-19-17-54-15-13-45-37(52)56-20-24-22-8-5-3-4-6-9-23(22)24/h21-25,32H,5-20H2,1-2H3,(H,45,52)(H,46,49)(H,47,48)(H3,43,44,51)/t22-,23+,24?,25-,32-/m0/s1
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| Chemical Name |
(2,3,4,5,6-pentafluorophenyl) (2S)-2-[[(2S)-2-[3-[2-[2-[2-[[(1S,8R)-9-bicyclo[6.1.0]non-4-ynyl]methoxycarbonylamino]ethoxy]ethoxy]ethoxy]propanoylamino]-3-methylbutanoyl]amino]-5-(carbamoylamino)pentanoate
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| Synonyms |
BCNPEG3VCPFP ester; BCN PEG3 VC PFP ester; BCN-PEG3-VC-PFP Ester; 2353409-45-5; 2,3,4,5,6-pentafluorophenyl (2S)-2-[(2S)-2-{3-[2-(2-{2-[({[(1R,8S,9S)-bicyclo[6.1.0]non-4-yn-9-yl]methoxy}carbonyl)amino]ethoxy}ethoxy)ethoxy]propanamido}-3-methylbutanamido]-5-(carbamoylamino)pentanoate; AKOS040743002; BP-24334; DA-71336;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.2198 mL | 6.0990 mL | 12.1979 mL | |
| 5 mM | 0.2440 mL | 1.2198 mL | 2.4396 mL | |
| 10 mM | 0.1220 mL | 0.6099 mL | 1.2198 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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