ALW-II-41-27
Based on 32 publication(s) in Google Scholar
ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 1186206-79-0
- Formula: C32H32F3N5O2S
- Molecular Weight:607.69
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) ALW-II-41-27
More- Signal Transduct Target Ther. 2022 Feb 2;7(1):33. [Abstract]
- Nat Commun. 2023 May 13;14(1):2756. [Abstract]
- Nat Commun. 2017 Jun 6;8:15729. [Abstract]
- J Neuroinflammation. 2025 Sep 24;22(1):211. [Abstract]
- Cell Death Dis. 2020 Aug 27;11(8):709. [Abstract]
- Cell Death Dis. 2018 Nov 19;9(12):1146. [Abstract]
- Mater Des. 2025 Oct 25;260:115016.
- Oncogene. 2017 Oct 5;36(40):5620-5630. [Abstract]
- Mol Cancer Ther. 2019 Apr;18(4):845-855. [Abstract]
- Cells. 2021 Oct 26;10(11):2893. [Abstract]
- Front Pharmacol. 2018 Mar 27:9:272. [Abstract]
- Int Immunopharmacol. 2024 Oct 9;143(Pt 1):113302. [Abstract]
- Mol Cancer Res. 2020 Nov;18(11):1735-1743. [Abstract]
- Int J Cancer. 2019 May 15;144(10):2440-2452. [Abstract]
- Int J Cancer. 2019 Nov 1;145(9):2440-2449. [Abstract]
- J Cell Mol Med. 2021 Mar;25(6):2967-2975. [Abstract]
- FASEB J. 2019 Dec;33(12):13644-13659. [Abstract]
- FASEB J. 2019 Apr;33(4):5495-5509. [Abstract]
- Sci Rep. 2026 Jan 25;16(1):6197. [Abstract]
- Sci Rep. 2024 Jan 17;14(1):1525. [Abstract]
- Heliyon. 2024 Dec 4;10(23):e40871. [Abstract]
- Breast Cancer Res Treat. 2020 Jan;179(2):337-347. [Abstract]
- J Cancer Res Clin Oncol. 2018 Sep;144(9):1649-1663. [Abstract]
- Cancer Manag Res. 2020 Dec 9:12:12667-12678. [Abstract]
- Oncol Lett. 2022 Apr;23(4):129. [Abstract]
- Oncol Lett. 2019 Sep;18(3):3031-3038. [Abstract]
- bioRxiv. 2026 Jan 5.
- bioRxiv. 2025 Aug 2:2025.07.31.667978. [Abstract]
- bioRxiv. 2025 Jun 16.
- Research Square Print. October 27th, 2022.
- bioRxiv. 2020 Apr.
- Oncotarget. 2017 Nov 1;8(61):104330-104346. [Abstract]
-
WB
-
WB
-
WB
-
WB
-
WB
Biological Activity
IC50: 11 nM (Eph2)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Bcr-Abl expressed in mouse BA/F3 cells
Inhibition of Tel fused Bcr-Abl expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Bmx expressed in mouse BA/F3 cells
Inhibition of Tel fused Bmx expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused EphA3 expressed in mouse BA/F3 cells
Inhibition of Tel fused EphA3 expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused FGR expressed in mouse BA/F3 cells
Inhibition of Tel fused FGR expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused FLT1 expressed in mouse BA/F3 cells
Inhibition of Tel fused FLT1 expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Fms expressed in mouse BA/F3 cells
Inhibition of Tel fused Fms expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused KDR expressed in mouse BA/F3 cells
Inhibition of Tel fused KDR expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Kit expressed in mouse BA/F3 cells
Inhibition of Tel fused Kit expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Lyn expressed in mouse BA/F3 cells
Inhibition of Tel fused Lyn expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
| BaF3 | EC50 |
<500 nM
Compound: 7
|
Inhibition of Tel fused Src expressed in mouse BA/F3 cells
Inhibition of Tel fused Src expressed in mouse BA/F3 cells
|
[PMID: 19553108] |
ALW-II-41-27 inhibits Ba/F3 cells transformed with Tel fusions of EphA3, Kit, Fms, KDR, FLT1, FGR, Src, Lyn, Bmx, and Bcr-Abl with an EC50 below 500 nM. ALW-II-41-27 exhibits cross reactivity with Bcr-Abl. ALW-II-41-27 inhibits b-raf, CSF1R, DDR1, DDR2, EphA2, EphA5, EphA8, EphB1, EphB2, EphB3, Frk, Kit, Lck, p38α, p38β, PDGFRα, PDGFRβ, and Raf1 and many more demonstrating how introduction of the thiophene group can have a tremendous impact on kinase selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1186206-79-0
-
Appearance Solid
-
Molecular Weight 607.69
-
Formula C32H32F3N5O2S
-
Color White to light yellow
-
SMILES
CC1=C(NC(C2=CC(C3=CC=CS3)=CN=C2)=O)C=C(C(NC4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4)=O)C=C1
-
Synonyms
Eph receptor tyrosine kinase inhibitor
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (32)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
EPHA2 mediates PDGFA activity and functions together with PDGFRA as prognostic marker and therapeutic target in glioblastoma. [Abstract]2022 Feb 2;7(1):33. PMID: 35105853 -
Nat Commun
Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis. [Abstract]2023 May 13;14(1):2756. PMID: 37179400 -
Nat Commun
Small extracellular vesicles secreted from senescent cells promote cancer cell proliferation through EphA2. [Abstract]2017 Jun 6;8:15729. PMID: 28585531
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 6;8:15729. [Abstract]
EphA2 immunoprecipitates prepared from MCF-7 cells expressing ectopic EphA2 are immunoblotted with anti-phosphotyrosine and anti-EphA2 antibody. The indicated samples are treated with recombinant human ephrin-A1 (500 ng/mL) for 20 min. Eight-hour pre-treatment with the EphA2 inhibitor ALW-II-41-27 (100 nM) suppressed ephrin-A1-induced EphA2 phosphorylation.
-
J Neuroinflammation
Inhibition of Ephrin receptor signaling in the paraventricular nucleus attenuates psoriasis-like dermatitis via synaptic plasticity and immune homeostasis modulation. [Abstract]2025 Sep 24;22(1):211. PMID: 40993793 -
Cell Death Dis
Y772 phosphorylation of EphA2 is responsible for EphA2-dependent NPC nasopharyngeal carcinoma growth by Shp2/Erk-1/2 signaling pathway. [Abstract]2020 Aug 27;11(8):709. PMID: 32848131 -
Cell Death Dis
EPH receptor A2 governs a feedback loop that activates Wnt/β-catenin signaling in gastric cancer. [Abstract]2018 Nov 19;9(12):1146. PMID: 30451837 -
-
Oncogene
Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers. [Abstract]2017 Oct 5;36(40):5620-5630. PMID: 28581527
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 Oct 5;36(40):5620-5630. [Abstract]
C3-TAg cells are starved and stimulated for 0, 15 and 30 min with ephrin-A1-Fc (EphA2 ligand; 1 μg/mL) in the presence or absence of ALW-II-41-27 or NG-25 control. EphA2 is immunoprecipitated and products probed for tyrosine phosphorylation and EphA2. ALW-II-41-27 significantly reduces basal and ephrin-A1-Fc induced tyrosine phosphorylation.
-
Mol Cancer Ther
EPHA2 Is a Predictive Biomarker of Resistance and a Potential Therapeutic Target for Improving Antiepidermal Growth Factor Receptor Therapy in Colorectal Cancer. [Abstract]2019 Apr;18(4):845-855. PMID: 30824612 -
Cells
EphA2 Expression in Bone Sarcomas: Bioinformatic Analyses and Preclinical Characterization in Patient-Derived Models of Osteosarcoma, Ewing's Sarcoma and Chondrosarcoma. [Abstract]2021 Oct 26;10(11):2893. PMID: 34831119 -
Front Pharmacol
A Novel EphA2 Inhibitor Exerts Beneficial Effects in PI-IBS in Vivo and in Vitro Models via Nrf2 and NF-κB Signaling Pathways. [Abstract]2018 Mar 27:9:272. PMID: 29662452
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Mar 27:9:272. [Abstract]
ALW-II-41-27 activates Nrf2 signaling whereas inhibits NF-kB signaling in Trichinella spiralis-infected mice.
-
Int Immunopharmacol
Icariin suppresses osteogenic differentiation and promotes bone regeneration in Porphyromonas gingivalis-infected conditions through EphA2-RhoA signaling pathway. [Abstract]2024 Oct 9;143(Pt 1):113302. PMID: 39388889 -
Mol Cancer Res
Phosphorylation of PLCγ1 by EphA2 Receptor Tyrosine Kinase Promotes Tumor Growth in Lung Cancer. [Abstract]2020 Nov;18(11):1735-1743. PMID: 32753469 -
Int J Cancer
Mutated EPHA2 is a target for combating lymphatic metastasis in intrahepatic cholangiocarcinoma. [Abstract]2019 May 15;144(10):2440-2452. PMID: 30412282 -
Int J Cancer
EPHA2 blockade reverses acquired resistance to afatinib induced by EPHA2-mediated MAPK pathway activation in gastric cancer cells and avatar mice. [Abstract]2019 Nov 1;145(9):2440-2449. PMID: 30957241 -
J Cell Mol Med
2021 Mar;25(6):2967-2975. PMID: 33586348 -
FASEB J
EphrinB2/ephB2-mediated myenteric synaptic plasticity: mechanisms underlying the persistent muscle hypercontractility and pain in postinfectious IBS. [Abstract]2019 Dec;33(12):13644-13659. PMID: 31601124 -
FASEB J
Dynamic membrane proteome of adipogenic and myogenic precursors in skeletal muscle highlights EPHA2 may promote myogenic differentiation through ERK signaling. [Abstract]2019 Apr;33(4):5495-5509. PMID: 30668921
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Apr;33(4):5495-5509. [Abstract]
Western analysis of p-EPHA2, EPAH2, p-AKT, AKT, P-ERK, ERK protein expression in the treatment of ALW-II-41-27 or transfected with siEPHA2 in GM before myogenic differentiation.
-
Sci Rep
Targeting the Akt-EphA2 axis and cell-cell adhesion enhances anoikis sensitivity in cancer cells. [Abstract]2026 Jan 25;16(1):6197. PMID: 41582276 -
Sci Rep
Cooperative function of oncogenic MAPK signaling and the loss of Pten for melanoma migration through the formation of lamellipodia. [Abstract]2024 Jan 17;14(1):1525. PMID: 38233537 -
Heliyon
A multi-model approach identifies ALW-II-41-27 as a promising therapy for osteoarthritis-associated inflammation and endochondral ossification. [Abstract]2024 Dec 4;10(23):e40871. PMID: 39717596 -
Breast Cancer Res Treat
2020 Jan;179(2):337-347. PMID: 31655920 -
J Cancer Res Clin Oncol
Cancer-associated fibroblasts promote gastric tumorigenesis through EphA2 activation in a ligand-independent manner. [Abstract]2018 Sep;144(9):1649-1663. PMID: 29948146
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2018 Sep;144(9):1649-1663. [Abstract]
Western blot analysis of E-cadherin, Cytokeratin, N-cadherin and Snail in AGS cells treated with 1 µM of ALW-II-41-27.
-
Cancer Manag Res
Quantitative Tyrosine Phosphoproteomic Analysis of Resistance to Radiotherapy in Nasopharyngeal Carcinoma Cells. [Abstract]2020 Dec 9:12:12667-12678. PMID: 33328764 -
Oncol Lett
ALW-II-41-27, an EphA2 inhibitor, inhibits proliferation, migration and invasion of cervical cancer cells via inhibition of the RhoA/ROCK pathway. [Abstract]2022 Apr;23(4):129. PMID: 35251349 -
Oncol Lett
Role of EphA2-PI3K signaling in vasculogenic mimicry induced by cancer-associated fibroblasts in gastric cancer cells. [Abstract]2019 Sep;18(3):3031-3038. PMID: 31452781 -
-
bioRxiv
2025 Aug 2:2025.07.31.667978. PMID: 40766426 -
-
-
-
Oncotarget
EphA2 signaling is impacted by carcinoembryonic antigen cell adhesion molecule 1-L expression in colorectal cancer liver metastasis in a cell context-dependent manner. [Abstract]2017 Nov 1;8(61):104330-104346. PMID: 29262644
ALW-II-41-27 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 1;8(61):104330-104346. [Abstract]
MC38-CT or -CC1-L cells are treated with 1 μM of DMSO, or the non-specific NG-25 or specific ALW-II-41-27 EPHA2 receptor inhibitor for indicated periods of time, followed by stimulation with EFNA1-Fc (2 μg/mL) in the last 15 min of treatments. Protein lysates are prepared and subjected to immunoblotting using antibodies to determine the effect of kinase inhibitors on EPHA2 activation.
Solvent & Solubility
DMSO : ≥ 47 mg/mL (77.34 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (4.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (275 KB)
-
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)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Choi, et al. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2009), 19(15), 4467-4470. [Content Brief]
[2]. Song W, et al. Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers. Oncogene. 2017 Jun 5. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6456 mL | 8.2279 mL | 16.4558 mL | 41.1394 mL |
| 5 mM | 0.3291 mL | 1.6456 mL | 3.2912 mL | 8.2279 mL | |
| 10 mM | 0.1646 mL | 0.8228 mL | 1.6456 mL | 4.1139 mL | |
| 15 mM | 0.1097 mL | 0.5485 mL | 1.0971 mL | 2.7426 mL | |
| 20 mM | 0.0823 mL | 0.4114 mL | 0.8228 mL | 2.0570 mL | |
| 25 mM | 0.0658 mL | 0.3291 mL | 0.6582 mL | 1.6456 mL | |
| 30 mM | 0.0549 mL | 0.2743 mL | 0.5485 mL | 1.3713 mL | |
| 40 mM | 0.0411 mL | 0.2057 mL | 0.4114 mL | 1.0285 mL | |
| 50 mM | 0.0329 mL | 0.1646 mL | 0.3291 mL | 0.8228 mL | |
| 60 mM | 0.0274 mL | 0.1371 mL | 0.2743 mL | 0.6857 mL |