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| Targets |
SC-VC-PAB-MMAE targets tubulin, a key component of the cytoskeleton involved in cell division. The anti-mitotic agent MMAE inhibits tubulin polymerization, disrupting microtubule dynamics and causing cell cycle arrest and apoptosis. The compound does not have a direct target itself but delivers MMAE to target cells when conjugated to an antibody. The cleavable linker SC-VC-PAB is designed to be cleaved in the tumor microenvironment, releasing MMAE.
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| ln Vitro |
In vitro, SC-VC-PAB-MMAE functions as a potent antitumor agent when delivered as part of an ADC. The MMAE payload inhibits tubulin polymerization, disrupting microtubule dynamics and causing cell cycle arrest and apoptosis. The activity of SC-VC-PAB-MMAE is evaluated in cell-based assays using ADC constructs. The compound's potency is assessed by measuring cell viability and proliferation in cancer cell lines. The cleavable linker enables selective drug release in the tumor microenvironment.
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| ln Vivo |
In vivo, SC-VC-PAB-MMAE has potent antitumor activity when used in ADCs. The ADC targets cancer cells through antibody-mediated recognition, delivering MMAE selectively to tumor tissues. The cleavable linker SC-VC-PAB enables drug release in the tumor microenvironment, minimizing systemic toxicity. In vivo efficacy is evaluated in mouse xenograft models of cancer. Tumor growth inhibition and survival are measured. However, specific data for this particular conjugate are not extensively detailed in the available literature.
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| Enzyme Assay |
Cell-free assays for SC-VC-PAB-MMAE involve characterizing its chemical properties and evaluating its ability to inhibit tubulin polymerization. Tubulin polymerization assays are performed using purified tubulin protein. The compound's ability to inhibit microtubule assembly is measured spectrophotometrically. The cleavable linker's susceptibility to cleavage in tumor-relevant conditions can be assessed using HPLC or LC-MS. Chemical purity and identity are confirmed by HPLC and mass spectrometry.
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| Cell Assay |
In vitro cellular assays for SC-VC-PAB-MMAE are performed using ADC constructs containing the drug-linker conjugate. Cancer cell lines expressing the target antigen are treated with the ADC at various concentrations. Cell viability is assessed using MTT, CellTiter-Glo, or other standard assays. Cell cycle analysis and apoptosis assays are performed to evaluate the mechanism of action. The specificity of the ADC is assessed by comparing activity in target-positive versus target-negative cell lines.
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| Animal Protocol |
In vivo animal studies for SC-VC-PAB-MMAE are conducted in mouse xenograft models of cancer using ADCs containing this drug-linker conjugate. The ADC is administered via intravenous injection. Tumor growth is monitored by measuring tumor volume using calipers. Pharmacokinetic parameters are determined from plasma samples. Efficacy is evaluated by comparing tumor growth rates and survival between treatment and control groups. However, specific protocols for this conjugate are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SC-VC-PAB-MMAE include a molecular weight of 1497.75 g/mol (approximate) and molecular formula C68H105N11O17 (approximate). The compound has a purity of ≥99%. As a drug-linker conjugate, its pharmacokinetic properties when incorporated into ADCs depend on the overall ADC structure. The compound is typically stored at appropriate conditions as a research reagent. Detailed ADME parameters are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of SC-VC-PAB-MMAE is related to the MMAE payload, which is a potent anti-mitotic agent with known toxicities including myelosuppression, neuropathy, and gastrointestinal effects. The cleavable linker is designed to minimize systemic toxicity by enabling targeted drug delivery. Standard toxicology studies would include assessment of acute and repeat-dose toxicity in rodent and non-rodent species. The compound is intended for research use only and not for therapeutic applications in humans.
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| References | |
| Additional Infomation |
SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for ADCs, consisting of the anti-mitotic agent MMAE linked via the cleavable linker SC-VC-PAB. MMAE inhibits tubulin polymerization, disrupting cell division. SC-VC-PAB-MMAE is a research tool for ADC development and cancer therapy research. It has not entered clinical trials as a standalone agent and is strictly for research purposes.
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| Molecular Formula |
C68H105N11O17
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|---|---|
| Molecular Weight |
1348.62481856346
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| Exact Mass |
1347.768
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| CAS # |
2259318-46-0
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| PubChem CID |
145712367
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
96
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| Complexity |
2580
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| Defined Atom Stereocenter Count |
12
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| SMILES |
O(C)[C@H]([C@H](C(N[C@H](C)[C@H](C1C=CC=CC=1)O)=O)C)[C@@H]1CCCN1C(C[C@H]([C@H]([C@@H](C)CC)N(C)C([C@H](C(C)C)NC([C@H](C(C)C)N(C(=O)OCC1C=CC(=CC=1)NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(CCCCC(=O)ON1C(CCC1=O)=O)=O)=O)=O)C)=O)=O)OC)=O
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| InChi Key |
IOJRSUDQDOZEEX-SBEKVBMRSA-N
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| InChi Code |
InChI=1S/C68H105N11O17/c1-15-42(8)59(50(93-13)37-54(83)78-36-22-26-49(78)61(94-14)43(9)62(86)71-44(10)60(85)46-23-17-16-18-24-46)76(11)66(90)57(40(4)5)75-65(89)58(41(6)7)77(12)68(92)95-38-45-29-31-47(32-30-45)72-63(87)48(25-21-35-70-67(69)91)73-64(88)56(39(2)3)74-51(80)27-19-20-28-55(84)96-79-52(81)33-34-53(79)82/h16-18,23-24,29-32,39-44,48-50,56-61,85H,15,19-22,25-28,33-38H2,1-14H3,(H,71,86)(H,72,87)(H,73,88)(H,74,80)(H,75,89)(H3,69,70,91)/t42-,43+,44+,48-,49-,50+,56-,57-,58-,59-,60+,61+/m0/s1
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 6-[[(2S)-1-[[(2S)-5-(carbamoylamino)-1-[4-[[[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-methylcarbamoyl]oxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-oxohexanoate
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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. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 (~74.15 mM)
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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 | 0.7415 mL | 3.7075 mL | 7.4149 mL | |
| 5 mM | 0.1483 mL | 0.7415 mL | 1.4830 mL | |
| 10 mM | 0.0741 mL | 0.3707 mL | 0.7415 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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