A-770041
Based on 7 publication(s) in Google Scholar
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection.
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- Purity: 99.89%
- CAS No.: 869748-10-7
- 화학식: C34H39N9O3
- 분자량:621.73
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
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HY-L039
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Publications Citing Use of MedChemExpress (MCE) A-770041
More- Cancer Res. 2024 Jul 2;84(13):2109-2122. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100917. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):387-400. [Abstract]
- Biochem Pharmacol. 2025 Jul:237:116930. [Abstract]
- Metabolites. 2022 Aug 25;12(9):793. [Abstract]
- Cell Immunol. 2022 Jun;376:104531. [Abstract]
Biological Activity
IC50: 0.147 μM (Lck), 9.1 μM (Src), 14.1 μM (Fgr), 44.1 μM (Fyn)[1]
A-770041 selective inhibits Lck with an IC50 value of 0.147 μM, and inhibits other Src family kinase Src, Fgr, Fyn with IC50s of 9.1, 14.1 and 44.1 μM, respectively[1]. A-770041 (0-30 μM; 2 h) dose-dependently inhibits anti-CD3 induced IL-2 production with an EC50 value of 80 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Lewis rats[1]
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Dosage:2.5 mg/kg
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Administration:Intragastric administration; 2.5 mg/kg once
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Result:Showed an inhibition of concanavalin A-induced IL-2 with an in vivo EC50 value of 78 nM.
Chemical Information
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CAS No. 869748-10-7
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Appearance Solid
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분자량 621.73
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화학식 C34H39N9O3
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Color White to off-white
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SMILES
NC1=C2C(N([C@@H]3CC[C@@H](N4CCN(C(C)=O)CC4)CC3)N=C2C5=CC=C(NC(C6=CC7=C(C=CC=C7)N6C)=O)C(OC)=C5)=NC=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Res
CD106 in tumor-specific exhausted CD8+ T cells mediates immunosuppression by inhibiting TCR signaling. [Abstract]2024 Jul 2;84(13):2109-2122. PMID: 38635899 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Rep Med
CD28-CAR-T cell activation through FYN kinase signaling rather than LCK enhances therapeutic performance. [Abstract]2023 Feb 21;4(2):100917. PMID: 36696897 -
Acta Pharmacol Sin
An IgD-Fc-Ig fusion protein restrains the activation of T and B cells by inhibiting IgD-IgDR-Lck signaling in rheumatoid arthritis. [Abstract]2022 Feb;43(2):387-400. PMID: 33864023 -
Biochem Pharmacol
A novel IgD-FcδR blocker, IgD-Fc-Ig fusion protein, effectively alleviates abnormal activation of T cells the disease progression in systemic lupus erythematosus. [Abstract]2025 Jul:237:116930. PMID: 40194603 -
Metabolites
Blockade of Tyrosine Kinase, LCK Leads to Reduction in Airway Inflammation through Regulation of Pulmonary Th2/Treg Balance and Oxidative Stress in Cockroach Extract-Induced Mouse Model of Allergic Asthma. [Abstract]2022 Aug 25;12(9):793. PMID: 36144198 -
Cell Immunol
Lck signaling inhibition causes improvement in clinical features of psoriatic inflammation through reduction in inflammatory cytokines in CD4+ T cells in imiquimod mouse model. [Abstract]2022 Jun;376:104531. PMID: 35576719
용액&용해도
DMSO : 25 mg/mL (40.21 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (3.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Stachlewitz RF, et al.A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejection.J Pharmacol Exp Ther. 2005 Oct;315(1):36-41. [Content Brief]
[2]. Andrew Burchat, et al. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection Bioorganic & Medicinal Chemistry Letters Volume 16, Issue 1, 1 January 2006, Pages 118-122 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6084 mL | 8.0421 mL | 16.0842 mL | 40.2104 mL |
| 5 mM | 0.3217 mL | 1.6084 mL | 3.2168 mL | 8.0421 mL | |
| 10 mM | 0.1608 mL | 0.8042 mL | 1.6084 mL | 4.0210 mL | |
| 15 mM | 0.1072 mL | 0.5361 mL | 1.0723 mL | 2.6807 mL | |
| 20 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0105 mL | |
| 25 mM | 0.0643 mL | 0.3217 mL | 0.6434 mL | 1.6084 mL | |
| 30 mM | 0.0536 mL | 0.2681 mL | 0.5361 mL | 1.3403 mL | |
| 40 mM | 0.0402 mL | 0.2011 mL | 0.4021 mL | 1.0053 mL |
A-770041 Related Classifications
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