| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Topoisomerase; Camptothecins
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|---|---|
| References | |
| Additional Infomation |
For many years, microtubule-targeting agents (MTAs) have been studied as payloads for antibody-drug conjugates (ADCs). However, due to insufficient efficacy or significant toxicity, many ADCs have limited efficacy, prompting continuous exploration of novel MTA payloads for next-generation ADCs. In this study, we developed an ADC using the MTA eribulin (a derivative of the macrocyclic polyether natural product halicondolin B) as the payload. In vitro experiments showed that the eribulin ADC exhibited good potency and specificity using different linkers and two different conjugation methods. MORAb-202 is an investigational drug composed of a humanized anti-human folate receptor α (FRA) antibody, fastuzumab, conjugated to maleimide-PEG2-valine-citrulline-p-aminobenzylcarbamoyl-eribulin via a reduced interchain disulfide bond, with a drug-to-antibody ratio of 4.0. MORAb-202 exhibits excellent biophysical properties and broad activity against a variety of FRA-positive tumor cell lines. Its in vitro specificity is also enhanced compared to farletuzumab conjugated with a variety of other MTA payloads, including MMAE, MMAF, and the reducible maytansine linker-payload sulfo-SPDB-DM4. In FRA-positive human tumor cell line xenograft models and patient-derived tumor xenograft models, a single dose of MORAb-202 can induce a potent and durable antitumor response. These data support further investigation of MORAb-202 as a potential new therapy for FRA-positive cancers, with the novel MTA eribulin as the payload. [1]
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| Molecular Formula |
C42H44F4N6O10
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|---|---|
| Molecular Weight |
868.8
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| Exact Mass |
868.30550
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| CAS # |
2928571-45-1
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| PubChem CID |
169494470
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
62
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| Complexity |
1710
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C5[C@H](CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)NC(=O)OCC7=CC=C(C=C7)NC(=O)[C@H](C)NC(=O)[C@H](C(C)C)N)O.C(=O)(C(F)(F)F)O
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| InChi Key |
BEGBTWTZTSSNHK-TYUAWROFSA-N
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| InChi Code |
InChI=1S/C40H43FN6O8.C2HF3O2/c1-6-40(53)26-13-30-34-24(15-47(30)37(50)25(26)17-54-38(40)51)32-28(12-11-23-19(4)27(41)14-29(45-34)31(23)32)46-39(52)55-16-21-7-9-22(10-8-21)44-35(48)20(5)43-36(49)33(42)18(2)3;3-2(4,5)1(6)7/h7-10,13-14,18,20,28,33,53H,6,11-12,15-17,42H2,1-5H3,(H,43,49)(H,44,48)(H,46,52);(H,6,7)/t20-,28-,33-,40-;/m0./s1
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| Chemical Name |
[4-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]propanoyl]amino]phenyl]methyl N-[(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]carbamate;2,2,2-trifluoroacetic acid
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| Synonyms |
Val-Ala-PABC-Exatecan trifluoroacetate; Val-Ala-PABC-Exatecan (trifluoroacetate); 2928571-45-1;
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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: 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 :~50 mg/mL (~57.55 mM; with sonication)
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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 | 1.1510 mL | 5.7551 mL | 11.5101 mL | |
| 5 mM | 0.2302 mL | 1.1510 mL | 2.3020 mL | |
| 10 mM | 0.1151 mL | 0.5755 mL | 1.1510 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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