| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Angiopep-2-Cys targets the brain for drug delivery as a brain peptide carrier. Angiopep-2 is a peptide that can cross the blood-brain barrier via receptor-mediated transcytosis. The cysteine conjugation enables linkage of anticancer active molecules to the Angiopep-2 carrier. By combining anticancer agents with Angiopep-2, the conjugate enhances delivery to brain tumors and improves therapeutic efficacy.
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| ln Vitro |
In vitro activity of Angiopep-2-Cys is related to its function as a brain-targeted drug delivery carrier. The conjugation of anticancer active molecules with the Angiopep-2 peptide carrier can enhance their activity in brain cancer. The compound itself is a carrier rather than a pharmacologically active agent. Its activity is evaluated in the context of the anticancer payload being delivered.
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| ln Vivo |
In vivo activity of Angiopep-2-Cys is related to its function as a brain-targeted drug delivery carrier. The conjugation of anticancer active molecules with Angiopep-2 can enhance their efficacy in the treatment of brain cancer. Angiopep-2 crosses the blood-brain barrier via receptor-mediated transcytosis, enabling delivery of therapeutic payloads to brain tumors. Detailed in vivo data depend on the specific payload being delivered.
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| Enzyme Assay |
The in vitro receptor binding assay for Angiopep-2-Cys involves measuring its interaction with receptors on the blood-brain barrier that mediate transcytosis. Binding assays using cells expressing the low-density lipoprotein receptor-related protein (LRP) or other Angiopep-2 receptors may be performed. Surface plasmon resonance or cell-based uptake assays can be used to assess binding and internalization. Standard protocols include appropriate positive controls and vehicle controls.
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| Cell Assay |
In vitro cell-based assays for Angiopep-2-Cys are conducted using brain endothelial cell lines to evaluate blood-brain barrier transport. Cells are treated with the compound or its conjugates, and uptake and transcytosis are measured using fluorescently labeled or radiolabeled compounds. Cytotoxicity is evaluated using standard cell viability assays. The efficacy of anticancer payloads conjugated to Angiopep-2 is evaluated in brain cancer cell lines.
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| Animal Protocol |
In vivo animal studies for Angiopep-2-Cys are typically conducted using mouse models of brain cancer. Animals are administered conjugates of anticancer agents with Angiopep-2-Cys, and tumor growth inhibition, survival, and brain drug concentrations are evaluated. The ability of Angiopep-2 to cross the blood-brain barrier and deliver therapeutic payloads to brain tumors is assessed. Pharmacokinetic parameters are determined from plasma and brain tissue samples.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Angiopep-2-Cys include a molecular weight of 2404.61 g/mol and formula C107H154N30O32S. Solubility includes DMSO at 6 mg/mL. As a peptide carrier, it is subject to proteolytic degradation. Detailed pharmacokinetic parameters such as half-life and bioavailability depend on the specific payload being delivered. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for Angiopep-2-Cys is limited. As a research-use compound, standard safety precautions for handling should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
Angiopep-2-Cys is a conjugate of Angiopep-2 hydrochloride (a brain peptide carrier) and cysteine. Conjugation of anticancer agents with Angiopep-2 enhances their efficacy in brain cancer. It has MW 2404.61 and formula C107H154N30O32S. Solubility in DMSO at 6 mg/mL. CAS 906480-09-9. It is intended for research use only.
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| Molecular Formula |
C107H154N30O32S
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|---|---|
| Molecular Weight |
2404.6144824028
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| Exact Mass |
2404.109
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| CAS # |
906480-09-9
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| PubChem CID |
146160137
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| Appearance |
White to off-white solid powder
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| Density |
1.51±0.1 g/cm3(Predicted)
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| LogP |
-14.9
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| Hydrogen Bond Donor Count |
39
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| Hydrogen Bond Acceptor Count |
38
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| Rotatable Bond Count |
81
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| Heavy Atom Count |
170
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| Complexity |
5190
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| Defined Atom Stereocenter Count |
0
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| SMILES |
SCC(C(=O)O)NC(C(CC1C=CC(=CC=1)O)NC(C(CCC(=O)O)NC(C(CCC(=O)O)NC(C(C(C)O)NC(C(CCCCN)NC(C(CC1C=CC=CC=1)NC(C(CC(N)=O)NC(C(CC(N)=O)NC(C(CCCNC(=N)N)NC(C(CCCCN)NC(CNC(C(CCCNC(=N)N)NC(C(CO)NC(CNC(CNC(C(CC1C=CC(=CC=1)O)NC(C(CC1C=CC=CC=1)NC(C(CC1C=CC=CC=1)NC(C(C(C)O)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
NTEVJSCQHIRPSH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C107H154N30O32S/c1-56(139)87(112)103(166)135-75(46-60-22-10-5-11-23-60)98(161)131-73(45-59-20-8-4-9-21-59)97(160)129-71(47-61-28-32-63(141)33-29-61)90(153)120-51-82(145)119-52-83(146)123-78(54-138)102(165)124-65(26-16-42-117-106(113)114)89(152)121-53-84(147)122-66(24-12-14-40-108)91(154)125-68(27-17-43-118-107(115)116)92(155)133-76(49-80(110)143)101(164)134-77(50-81(111)144)100(163)132-72(44-58-18-6-3-7-19-58)96(159)126-67(25-13-15-41-109)95(158)137-88(57(2)140)104(167)128-70(37-39-86(150)151)93(156)127-69(36-38-85(148)149)94(157)130-74(48-62-30-34-64(142)35-31-62)99(162)136-79(55-170)105(168)169/h3-11,18-23,28-35,56-57,65-79,87-88,138-142,170H,12-17,24-27,36-55,108-109,112H2,1-2H3,(H2,110,143)(H2,111,144)(H,119,145)(H,120,153)(H,121,152)(H,122,147)(H,123,146)(H,124,165)(H,125,154)(H,126,159)(H,127,156)(H,128,167)(H,129,160)(H,130,157)(H,131,161)(H,132,163)(H,133,155)(H,134,164)(H,135,166)(H,136,162)(H,137,158)(H,148,149)(H,150,151)(H,168,169)(H4,113,114,117)(H4,115,116,118)
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| Chemical Name |
4-[[2-[[2-[[6-amino-2-[[2-[[4-amino-2-[[4-amino-2-[[2-[[6-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[(2-amino-3-hydroxybutanoyl)amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]-4-oxobutanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[1-[(1-carboxy-2-sulfanylethyl)amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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, avoid exposure to moisture. |
| 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 :~10 mg/mL (~4.16 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 | 0.4159 mL | 2.0793 mL | 4.1587 mL | |
| 5 mM | 0.0832 mL | 0.4159 mL | 0.8317 mL | |
| 10 mM | 0.0416 mL | 0.2079 mL | 0.4159 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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