Name: ALW-II-41-27
Brand: GlpBio
SKU: GC11134
Availability: InStock
Rating: 5 (30 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Cell experiment [1]:
Cell lines	Non-small cell lung cancer (NSCLC) PC-9/ER, PC-9/ERC15, PC-9/ERC16 cell lines
Preparation Method	Four cell lines with acquired resistance to erlotinib were treated with ALW-II-41-27, NG-25, erlotinib, or DMSO for 72 hours, and cell viability was assessed by the MTT assay.
Reaction Conditions	1 µM;72 h
Applications	1 µM ALW-II-41-27 inhibited the proliferation of Erlotinib-resistant NSCLC cell lines and increased cell apoptosis. ALW-II-41-27 induced apoptosis was accompanied by an increase in caspase-3 and PARP and a decrease in the expression of anti-apoptotic proteins BCL-xL and MCL-1.
Animal experiment [2]:
Animal models	6-week-old athymic nude mice
Preparation Method	HCC827/ER or PC-9/ERC16 cells were injected with Matrigel into the hind flanks of 6-week-old athymic nude mice. Mice were randomized by body weight and tumor volume into treatment groups to receive 15 mg/kg of either erlotinib, ALW-II-41-27, or the vehicle alone twice daily via intraperitoneal injection.
Dosage form	15 mg/kg;14 days; i.p.
Applications	After 14 days of the treatment regimen, ALW-II-41-27 significantly inhibited growth of the erlotinib-resistant tumors.
References: [1]. Amato KR, Wang S, et,al. EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Res. 2016 Jan 15;76(2):305-18. doi: 10.1158/0008-5472.CAN-15-0717. Epub 2016 Jan 7. PMID: 26744526; PMCID: PMC4715957.

ALW-II-41-27 is an Eph family tyrosine kinase inhibitor with an IC50 of 11 nM to inhibit Eph2^[1].

ALW-II-41-27(1μM;72 h) inhibited the proliferation of Erlotinib-resistant NSCLC cell lines and increased cell apoptosis. ALW-II-41-27 induced apoptosis was accompanied by an increase in caspase-3 and PARP and a decrease in the expression of anti-apoptotic proteins BCL-xL and MCL-1^[3]. ALW-II-41-27(200, 600 or 1,000 nM ALW-II-41-27; 24, 48 or 72 h) inhibited cervical cancer (CC) cell proliferation, migration and invasion by blocking the RhoA/ROCK pathway^[4]. ALW-II-41-27 inhibited pY772-EphA2 and EphA2-Y772A decreased the inhibitory effect of ALW-II-41-27 on NPC cell proliferation^[6]. Combined treatment with ALW-II-41-27 plus cetuximab reverted primary and acquired resistance to cetuximab, causing cell growth inhibition, inducing apoptosis and cell-cycle G1-G2 arrest^[7].

ALW-II-41-27(15 mg/kg;14 days; i.p.) significantly inhibited growth of the erlotinib-resistant tumors^[3]. Administration of ALW-II-41-27(15, 30 mg/kg;twice a day; i.p.)significantly inhibited H358 tumor growth in tumor-bearing mice. Histological analysis showed a significant increase in apoptosis in tumors treated with ALW-II-41-27 compared with those treated with NG-25 or the carrier, similar to the effect of genetic ablation of EPHA2^[2]. ALW-II-41-27 (12.5, 25, 50, and 100 μg/kg; i.p.) decreased gastrointestinal motility and abdominal withdrawal reflex (AWR) scores, markedly reduced the levels of oxidative stress markers [4-hydroxy-2-nonenal (4-HNE), protein carbonyl, and 8-hydroxy-2-de-axyguanine (8-OHdG)] and proinflammatory cytokines (TNF-α, IL-6, IL-17, and ICAM-1), and remarkably increased the level of anti-inflammatory cytokine (IL-10) in serum and colon of Trichinella spiralis-infected mice^[5].

References:
[1]. Choi Y, Syeda F, et,al. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4467-70. doi: 10.1016/j.bmcl.2009.05.029. Epub 2009 May 13. PMID: 19553108; PMCID: PMC2730633.
[2]. Amato KR, Wang S, et,al. Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. J Clin Invest. 2014 May;124(5):2037-49. doi: 10.1172/JCI72522. Epub 2014 Apr 8. PMID: 24713656; PMCID: PMC4001547.
[3]. Amato KR, Wang S, et,al. EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Res. 2016 Jan 15;76(2):305-18. doi: 10.1158/0008-5472.CAN-15-0717. Epub 2016 Jan 7. PMID: 26744526; PMCID: PMC4715957.
[4]. Li X, Li D, et,al.ALW-II-41-27, an EphA2 inhibitor, inhibits proliferation, migration and invasion of cervical cancer cells via inhibition of the RhoA/ROCK pathway. Oncol Lett. 2022 Apr;23(4):129. doi: 10.3892/ol.2022.13249. Epub 2022 Feb 18. PMID: 35251349; PMCID: PMC8895465.
[5]. Zeng L, Li K, et,al.A Novel EphA2 Inhibitor Exerts Beneficial Effects in PI-IBS in Vivo and in Vitro Models via Nrf2 and NF-κB Signaling Pathways. Front Pharmacol. 2018 Mar 27;9:272. doi: 10.3389/fphar.2018.00272. PMID: 29662452; PMCID: PMC5890185.
[6]. Xiang YP, Xiao T, et,al. Y772 phosphorylation of EphA2 is responsible for EphA2-dependent NPC nasopharyngeal carcinoma growth by Shp2/Erk-1/2 signaling pathway. Cell Death Dis. 2020 Aug 27;11(8):709. doi: 10.1038/s41419-020-02831-0. PMID: 32848131; PMCID: PMC7449971.
[7]. Martini G, Cardone C, et,al. EPHA2 Is a Predictive Biomarker of Resistance and a Potential Therapeutic Target for Improving Antiepidermal Growth Factor Receptor Therapy in Colorectal Cancer. Mol Cancer Ther. 2019 Apr;18(4):845-855. doi: 10.1158/1535-7163.MCT-18-0539. Epub 2019 Mar 1. PMID: 30824612.

Cas No.	1186206-79-0	SDF
Synonymes	Eph receptor tyrosine kinase inhibitor;
Chemical Name	N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide
Canonical SMILES	CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(C3=CC(NC(C4=CN=CC(C5=CC=CS5)=C4)=O)=C(C=C3)C)=O)C=C2)CC1
Formula	C₃₂H₃₂F₃N₅O₂S	M.Wt	607.69
Solubility	≥ 102 mg/mL in DMSO, ≥ 60.8 mg/mL in EtOH	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.6456 mL	8.2279 mL	16.4558 mL
	5 mM	0.3291 mL	1.6456 mL	3.2912 mL
	10 mM	0.1646 mL	0.8228 mL	1.6456 mL

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ALW-II-41-27 (Synonyms: Eph receptor tyrosine kinase inhibitor;)

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Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

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Dilution Calculator

In vivo Formulation Calculator (Clear solution)

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