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| 25mg |
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Purity: ≥98%
Atrasentan (ABT-627; NSC720763; A-147627; trade name: Xinlay) is a novel, selective and potent endothelin receptor/ET antagonist with anticancer activity. It suppresses ETA with an IC50 of 0.0551 nM. It's an experimental medication being researched to treat different cancers, including non-small cell lung cancer. Additionally, it's being looked into as a treatment for diabetic kidney disease. In patients who were not responding to hormone therapy, trasentan was not successful in a phase 3 trial for prostate cancer. Atrasentan is a medication that blocks the function of endothelin-1 and may be used to treat hormone-resistant prostate cancer that has metastasized.
| Targets |
ETA ( IC50 = 0.055 nM )
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| ln Vivo |
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| Enzyme Assay |
Atrasentan is used to treat and incubate the cells. After two PBS washes, they are lysed in an ice-cold lysis buffer [1 mM EGTA, 1 mM EDTA, 1.5 mM Tris (pH 7.4), 150 mM NaCl, 1% Triton X-100, 2.5 mM sodium PPi, 1 mM β-glycerophosphate, 1 mM sodium orthovanadate, 1 μg/mL leupeptin, and 1 mM PMSF]. After centrifuging the extracts to get rid of any remaining cell debris, the bicinchoninic acid (BCA) protein assay reagent is used to measure the amount of protein in the supernatants. Proteins (150 μg) cross-linked to agarose hydrazide beads and incubated with mild rocking at 4°C for the entire night. The lysis buffer and kinase assay buffer (25 mM Tris (pH 7.5), 10 mM MgCl2, 5 mM β-glycerol phosphate, 0.1 mM sodium orthovanadate, 2 mM DTT) are used to wash the immunoprecipitated products twice after Akt is selectively immunoprecipitated from the cell lysates. The products are then resuspended in 40 μL of kinase assay buffer that contains 200 μM ATP and 1 μg GSK-3α/β fusion protein. The addition of Lamelli SDS sample buffer stops the kinase assay reaction after it has been running for 30 minutes at 30°C. 10% SDS-PAGE is used to resolve the reaction products, and then an antiphosphorylated GSK-3α/β antibody is used for Western blotting. After separating 40 μg of protein from the lysate samples using 10% SDS-PAGE, anti-Akt antibody is used for Western blotting in order to determine the total amount of Akt.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C29H38N2O6
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| Molecular Weight |
510.62182
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| Exact Mass |
510.27
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| Elemental Analysis |
C, 68.21; H, 7.50; N, 5.49; O, 18.80
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| CAS # |
173937-91-2
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| Related CAS # |
Atrasentan hydrochloride; 195733-43-8; 178738-96-0 (sodium); 195704-72-4
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| Appearance |
Solid powder
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| SMILES |
CCCCN(CCCC)C(=O)CN1C[C@@H]([C@H]([C@@H]1C2=CC=C(C=C2)OC)C(=O)O)C3=CC4=C(C=C3)OCO4
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| InChi Key |
MOTJMGVDPWRKOC-QPVYNBJUSA-N
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| InChi Code |
InChI=1S/C29H38N2O6/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34)/t23-,27-,28+/m1/s1
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| Chemical Name |
(2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
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| Synonyms |
ABT-627; (+)-A 127722; ABT627; ABT 627; ABT-627; NSC720763; A147627; Abbott 147627; trade name: Xinlay; A-147627
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9584 mL | 9.7920 mL | 19.5840 mL | |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9168 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04573478 | Active Recruiting |
Drug: Atrasentan Drug: Placebo |
Immunoglobulin A Nephropathy IgA Nephropathy |
Chinook Therapeutics U.S., Inc. | December 11, 2020 | Phase 3 |
| NCT04573920 | Recruiting | Drug: Atrasentan | IgA Nephropathy Alport Syndrome |
Chinook Therapeutics U.S., Inc. | February 1, 2021 | Phase 2 |
| NCT05834738 | Active Recruiting |
Drug: Atrasentan Drug: Placebo |
Immunoglobulin A Nephropathy IgA Nephropathy |
Chinook Therapeutics, Inc. | July 20, 2023 | Phase 2 |
| NCT02118714 | Completed | Drug: Atrasentan | Nephropathy Diabetes |
AbbVie | April 6, 2015 | Phase 2 |
| NCT00181558 | Completed | Drug: Atrasentan Drug: Zoledronic Acid (Zometa) |
Adenocarcinoma of the Prostate Prostate Cancer |
Massachusetts General Hospital | December 2001 | Phase 2 |
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