Src Inhibitor 1
Based on 17 publication(s) in Google Scholar
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
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- Pureté: 99.97%
- CAS No.: 179248-59-0
- Formule: C22H19N3O3
- Masse moléculaire:373.40
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) Src Inhibitor 1
More- Bioact Mater. 2021 Jun 1:7:364-376. [Abstract]
- Mol Cell. 2023 Dec 7;83(23):4334-4351.e7. [Abstract]
- Theranostics. 2021 Jan 1;11(3):1473-1492. [Abstract]
- Adv Sci (Weinh). 2025 Oct 23:e11573. [Abstract]
- Cell Death Dis. 2025 Aug 7;16(1):595. [Abstract]
- Kardiol Pol. 2021;79(9):972-979. [Abstract]
- Ecotoxicol Environ Saf. 2025 Jul 15:300:118486. [Abstract]
- Int Immunopharmacol. 2022 Dec;113(Pt A):109340. [Abstract]
- mBio. 2026 Apr 8;17(4):e0389625. [Abstract]
- Cancers (Basel). 2026 Mar 26;18(7):1082. [Abstract]
- FASEB J. 2019 May;33(5):6254-6268. [Abstract]
- Ren Fail. 2024 Dec;46(1):2327498. [Abstract]
- J Pharm Pharmacol. 2021 Jul 7;73(8):1062-1070. [Abstract]
- Front Oncol. 2021 Jun 17:11:643669. [Abstract]
- Korean J Physiol Pharmacol. 2021 Mar 1;25(2):159-166. [Abstract]
- Res Sq. 2026 May 19.
- Research Square Preprint. 2020 Jun.
Customer Validation & Images
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Flow Cytometry
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WB
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WB
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Bio/Physico-chemical Assay
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Cell Migration/Invasion Assay
Activité biologique
IC50: 44 nM (Src), 88 nM (Lck)[1]
Src Inhibitor 1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src Inhibitor 1 is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 179248-59-0
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Appearance Solid
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Masse moléculaire 373.40
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Formule C22H19N3O3
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Color Off-white to yellow
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SMILES
COC1=CC2=NC=NC(NC3=CC=C(OC4=CC=CC=C4)C=C3)=C2C=C1OC
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Synonyms
Src Kinase Inhibitor 1; Src-l1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Bioact Mater
2021 Jun 1:7:364-376. PMID: 34466738 -
Mol Cell
EGFR promotes ALKBH5 nuclear retention to attenuate N6-methyladenosine and protect against ferroptosis in glioblastoma. [Abstract]2023 Dec 7;83(23):4334-4351.e7. PMID: 37979586 -
Theranostics
H3K27 acetylation activated-COL6A1 promotes osteosarcoma lung metastasis by repressing STAT1 and activating pulmonary cancer-associated fibroblasts. [Abstract]2021 Jan 1;11(3):1473-1492. PMID: 33391546
Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(3):1473-1492. [Abstract]
Src Inhibitor 1 (10 µM; 24 h) significantly suppressed the effect of COL6A1 overexpression on Src and FAK activation in OS cell lines, U2OS and Saos-2.
Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(3):1473-1492. [Abstract]
COL6A1-overexpressing OS cells and control cells were subjected to a cell-matrix adhesion assay to Col I, Col IV, and FN upon treatment with Src Inhibitor 1 (10 µM; 24 h).
Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(3):1473-1492. [Abstract]
Src Inhibitor 1 (10 µM; 24 h) significantly suppressed the effect of COL6A1 overexpression on the migration of OS cell lines, U2OS and Saos-2.
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Adv Sci (Weinh)
Chronic ER Stress Triggers Cell-Surface Chaperones as the Therapeutic Targets of CAR Cells in Acute Myeloid Leukemia. [Abstract]2025 Oct 23:e11573. PMID: 41126722
Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 23:e11573. [Abstract]
Src Inhibitor 1 (20 μM; 24 h) decreased cell-surface HSP90B1 expression in living MV4-11 and Molm13 cells.
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Cell Death Dis
Activation of AKT via a dual mechanism enhances the susceptibility of melanoma cells to glucose deprivation. [Abstract]2025 Aug 7;16(1):595. PMID: 40774947 -
Kardiol Pol
Src-IL-18 signaling regulates the secretion of atrial natriuretic factor in hypoxic beating rat atria. [Abstract]2021;79(9):972-979. PMID: 34176112 -
Ecotoxicol Environ Saf
Uncovering the effects of ATBC plasticizers on intracerebral hemorrhage outcomes based on network toxicology and in vitro and in vivo experimental validation. [Abstract]2025 Jul 15:300:118486. PMID: 40482445 -
Int Immunopharmacol
Blockade of JAK2 retards cartilage degeneration and IL-6-induced pain amplification in osteoarthritis. [Abstract]2022 Dec;113(Pt A):109340. PMID: 36330910
Src Inhibitor 1 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Dec;113(Pt A):109340. [Abstract]
SRC inhibitor 1 (5 μM) significantly reduces SRC phosphorylation in the mouse chondrocytes.
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mBio
ATP1A1 enhances porcine reproductive and respiratory syndrome virus type 2 attachment and internalization. [Abstract]2026 Apr 8;17(4):e0389625. PMID: 41773865 -
Cancers (Basel)
SFK Inhibition Suppresses EBV-Encoded BART miRNAs and Induces Apoptosis in EBV-Positive Gastric Epithelial Cells. [Abstract]2026 Mar 26;18(7):1082. PMID: 41976305 -
FASEB J
Transactivation domain of Krüppel-like factor 15 negatively regulates angiotensin II-induced adventitial inflammation and fibrosis. [Abstract]2019 May;33(5):6254-6268. PMID: 30776250 -
Ren Fail
Iguratimod prevents renal fibrosis in unilateral ureteral obstruction model mice by suppressing M2 macrophage infiltration and macrophage-myofibroblast transition. [Abstract]2024 Dec;46(1):2327498. PMID: 38666363 -
J Pharm Pharmacol
miR-424-5p reduces 5-fluorouracil resistance possibly by inhibiting Src/focal adhesion kinase signalling-mediated epithelial-mesenchymal transition in colon cancer cells. [Abstract]2021 Jul 7;73(8):1062-1070. PMID: 33793771 -
Front Oncol
Carcinoembryonic Antigen Related Cell Adhesion Molecule 6 Promotes Carcinogenesis of Gastric Cancer and Anti-CEACAM6 Fluorescent Probe Can Diagnose the Precancerous Lesions. [Abstract]2021 Jun 17:11:643669. PMID: 34221964 -
Korean J Physiol Pharmacol
NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria. [Abstract]2021 Mar 1;25(2):159-166. PMID: 33602886 -
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Solvant et solubilité
DMSO : 9.09 mg/mL (24.34 mM; Need ultrasonic; 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.91 mg/mL (2.44 mM); Clear solution
This protocol yields a clear solution of ≥ 0.91 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 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.
Protocole
Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (281 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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Instruction de manipulation (2659 KB)
Références
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91. [Content Brief]
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6781 mL | 13.3905 mL | 26.7809 mL | 66.9523 mL |
| 5 mM | 0.5356 mL | 2.6781 mL | 5.3562 mL | 13.3905 mL | |
| 10 mM | 0.2678 mL | 1.3390 mL | 2.6781 mL | 6.6952 mL | |
| 15 mM | 0.1785 mL | 0.8927 mL | 1.7854 mL | 4.4635 mL | |
| 20 mM | 0.1339 mL | 0.6695 mL | 1.3390 mL | 3.3476 mL |
Src Inhibitor 1 Related Classifications
HY-101053 Related Classifications
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