| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ln Vivo |
In comparison to free paclitaxel, ANG1005 exhibits much better brain delivery and brain metastases in breast cancer [1].
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| References |
[1]. Thomas FC, et al. Uptake of ANG1005, a novel paclitaxel derivative, through the blood-brain barrier into brain and experimental brain metastases of breast cancer. Pharm Res. 2009 Nov;26(11):2486-94.
[2]. Li F, et al. Targeting metastatic breast cancer with ANG1005, a novel peptide-paclitaxel conjugate that crosses the blood-brain-barrier (BBB). Genes Dis. 2017 Feb 10;4(1):1-3. [3]. Kumthekar P, et al. ANG1005, a Brain-Penetrating Peptide-Drug Conjugate, Shows Activity in Patients with Breast Cancer with Leptomeningeal Carcinomatosis and Recurrent Brain Metastases. Clin Cancer Res. 2020 Jun 15;26(12):2789-2799. |
| Additional Infomation |
Three paclitaxel molecules linked by a cleavable succinyl ester linkage to a brain peptide vector, Angiopep-2, conjugate named ANG1005.
Paclitaxel Trevatide is a peptide-drug conjugate containing the taxane paclitaxel covalently linked to the proprietary 19 amino acid peptide angiopep-2, in a 3:1 ratio, with potential antineoplastic activity. Upon administration, paclitaxel trevatide, via angiopep-2 moiety, binds to LRP-1 (low density lipoprotein receptor-related protein 1), which is highly expressed in blood brain barrier (BBB) and glioma cells. This binding allows the transcytosis of the agent across the BBB and the delivery of the cytotoxic agent paclitaxel. Compared to paclitaxel alone, GRN1005 is able to increase the concentration of paclitaxel in the brain and is also able to specifically deliver paclitaxel to LRP-1-overexpressing tumor cells, both in the brain and in the periphery. Drug Indication Investigated for use/treatment in brain cancer. |
| Molecular Formula |
C259H311N33O80
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|---|---|
| Molecular Weight |
5166.41381192207
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| CAS # |
1075214-55-9
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| PubChem CID |
46884921
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
46
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| Hydrogen Bond Acceptor Count |
81
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| Rotatable Bond Count |
138
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| Heavy Atom Count |
368
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| Complexity |
14000
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| Defined Atom Stereocenter Count |
50
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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: 100 mg/mL (19.50 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 | 0.1936 mL | 0.9678 mL | 1.9356 mL | |
| 5 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | |
| 10 mM | 0.0194 mL | 0.0968 mL | 0.1936 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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