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Results for "

ALK mutation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (12) Akt (2) Apoptosis (4) Autophagy (1) Cytochrome P450 (1) EGFR (2) ERK (2) Ligands for Target Protein for PROTAC (1) p38 MAPK (1) PROTACs (2) ROS Kinase (1)
By Research Areas:	Cancer (13)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-135887

ZX-29	Anaplastic lymphoma kinase (ALK) Apoptosis Autophagy	Cancer
ZX-29 is a potent and selective *ALK* inhibitor with an IC₅₀ of 2.1 nM, 1.3 nM and 3.9 nM for *ALK, ALK* L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an *ALK* mutation. ZX-29 also induces protective autophagy and has antitumor effect .

HY-12857

Brigatinib 25+ Cited Publications AP-26113	Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC .

HY-139279

Zotizalkib 3 Publications Verification TPX-0131	Anaplastic lymphoma kinase (ALK)	Cancer
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC₅₀ of 1.4 nM) and **ALK-resistant mutation, e.g. G1202R (IC₅₀ of 0.3 nM), L1196M (IC₅₀** of 0.3 nM). Zotizalkib has strong antitumor activities .

HY-146408

ALK-IN-21	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-21 (Compound B10), a potent *ALK* inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC₅₀ values of 4.59 nM, 2.07 nM and 5.95 nM toward ALK ^WT, ALK ^L1196M and ALK ^G1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC₅₀ values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma .

HY-12857R

Brigatinib (Standard)	Anaplastic lymphoma kinase (ALK)	Cancer
Brigatinib (Standard) is the analytical standard of Brigatinib. This product is intended for research and analytical applications. Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC .

HY-105369

KF-20444	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
KF-20444 is an orally active *ALK* inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against *ALK* fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .

HY-174315

WZH-17-002	PROTACs Anaplastic lymphoma kinase (ALK) Akt ERK	Cancer
WZH-17-002 is a WZH-15-125-based *ALK* PROTAC degrader with a DC₅₀ of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)

HY-146022

SIAIS117	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer .

HY-174314

WZH-15-125	Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK)	Cancer
WZH-15-125 is a potent *ALK* inhibitor. WZH-15-125 can effectively overcome drug resistance, especially compound *ALK* mutations. WZH-15-125 has an IC₅₀ of 101.7 nM for the highly refractory G1202R/L1196M mutation that is resistant to Lorlatinib (HY-12215). WZH-15-125 can be used as a PROTAC target protein ligand to synthesize PROTAC WZH-17-002 (HY-174315). WZH-15-125 can be used in the research of non-small cell lung cancer .

HY-170928

DA-0157	EGFR Anaplastic lymphoma kinase (ALK) Cytochrome P450	Cancer
DA-0157 is the orally active inhibitor for EGFR and *ALK* that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC₅₀ = 6.9 nM), Ba/F3-EGFR WT (IC₅₀ = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC₅₀ = 5.5 nM), and Ba/F3-EML4-ALK (IC₅₀ = 7.4 nM). DA-0157 inhibits CYP2D6 with IC₅₀ of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .

HY-W814315

Alectinib analog CH5424802 analog; RO5424802 analog; RG7853 analog	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitory activity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model .

HY-178391

SMU-037	ROS Kinase p38 MAPK ERK Apoptosis	Cancer
SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .

HY-178057

EGFR-IN-176	EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of *ALK* (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .

Cat. No.	Product Name

HY-L075

Anti-Lung Cancer Compound Library	2,521 compounds
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers. As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy. MCE offers a unique collection of 2,521 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Anti-Lung Cancer Compound Library

2,521 compounds

Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.

As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.

MCE offers a unique collection of 2,521 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

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