SGI-7079
Based on 3 publication(s) in Google Scholar
SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].
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- Purity: 99.32%
- CAS No.: 1239875-86-5
- 화학식: C26H26FN7
- 분자량:455.53
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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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Kinase Inhibitor Library
HY-L009
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NF-κB Signaling Compound Library
HY-L014
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) SGI-7079
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Customer Validation & Images
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WB
Biological Activity
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Axl |
SGI-7079 significantly inhibits the proliferation of SUM149 and KPL-4 breast cancer cells with IC50 of 0.43 μM and 0.16 μM at 72 h, respectively[1].
SGI-7079 (0.25 μM, 0.5 μM; 18 h) significantly reduces the migration and invasion abilities of SUM149 cells[1].
SGI-7079 (1 μM; 5 h) blocks Gas6-induced Axl (Tyr702) phosphorylation[1].
SGI-7079 (0.25 μM, 0.5 μM; 48 h) inhibits cell cycle arrest at G1/S phase in KPL-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SGI-7079 (50 mg/kg; oral; 5 days a week for 2 weeks) combined with anti-PD-1 antibody, induces tumor eradication in the mouse ID8 ovarian cancer peritoneal model, with one-third of the mice surviving long-term[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1239875-86-5
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Appearance Solid
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분자량 455.53
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화학식 C26H26FN7
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Color Light yellow to yellow
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SMILES
N#CCC1=CC=CC(C2=C3C(NC=C3C)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1
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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 (3)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Anlotinib combined with osimertinib reverses acquired osimertinib resistance in NSCLC by targeting the c-MET/MYC/AXL axis. [Abstract]2023 Jan 18;188:106668. PMID: 36681369
SGI-7079 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Jan 18;188:106668. [Abstract]
SGI-7079 (1 μM; 24 h) effectively inhibits AXL activation in HCC827/OR and H1975/OR cells.
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Antimicrob Agents Chemother
Repurposing Axl Kinase Inhibitors for the Treatment of Respiratory Syncytial Virus Infection. [Abstract]2023 Mar 16;67(3):e0148722. PMID: 36853000 -
용액&용해도
DMSO : ≥ 34 mg/mL (74.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.17 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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]. Wang X, et al. TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase. Cancer Res. 2013 Nov 1;73(21):6516-25. [Content Brief]
[2]. Wang SC, et al. Chidamide and mitomycin C exert synergistic cytotoxic effects against bladder cancer cells in vitro and suppress tumor growth in a rat bladder cancer model. Cancer Lett. 2022 Apr 1;530:8-15 [Content Brief]
[3]. Guo Z, et al. Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models. Oncotarget. 2017 Sep 21;8(52):89761-89774. [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 | 2.1952 mL | 10.9762 mL | 21.9525 mL | 54.8811 mL |
| 5 mM | 0.4390 mL | 2.1952 mL | 4.3905 mL | 10.9762 mL | |
| 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL | 5.4881 mL | |
| 15 mM | 0.1463 mL | 0.7317 mL | 1.4635 mL | 3.6587 mL | |
| 20 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7441 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8781 mL | 2.1952 mL | |
| 30 mM | 0.0732 mL | 0.3659 mL | 0.7317 mL | 1.8294 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3720 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0976 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3659 mL | 0.9147 mL |
SGI-7079 Related Classifications
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