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EML4-ALK

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (18) Akt (1) Apoptosis (6) Cytochrome P450 (1) EGFR (2) ERK (1) FKBP (1) PROTACs (5) Reference Standards (1) ROS Kinase (3) Trk Receptor (1)
By Research Areas:	Cancer (20)

Targets Recommended: Anaplastic lymphoma kinase (ALK)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111752

EML4-ALK kinase inhibitor 1	Anaplastic lymphoma kinase (ALK)	Cancer
EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase *(EML4-ALK), with an IC₅₀* of 1 nM .

HY-112140

JH-VIII-157-02	Anaplastic lymphoma kinase (ALK)	Cancer
JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC₅₀ of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

HY-164397

XMU-MP-5	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC₅₀s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .

HY-153386

CPD-1224	Anaplastic lymphoma kinase (ALK)	Cancer
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .

HY-174368

*PROTAC EML4-ALK Degrader-1* Pro-BA	PROTACs Apoptosis Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC₅₀ of 74 nM in H1322 cells (T_1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer. (Pink: EML4-ALK Ligand (HY-40114); Blue: GID4 Ligand (HY-150908))

HY-161910

SH-E4A-66	Anaplastic lymphoma kinase (ALK)	Cancer
SH-E4A-66 is a C ²-COUPLr (COvalent Protein Ligator) with carbazole scaffold barring heterogeneous cysteine reactive warheads (acrylamide and chloroacetamide). SH-E4A-66 is capable of coupling with *EML4-ALK* (EC₅₀=1.5 μM) and inhibiting the activity of *EML4-ALK* kinase (IC₅₀=2.3 μM) .

HY-161749

PROTAC ALK degrader-1	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC₅₀ of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .

HY-170592

dALK-3	Anaplastic lymphoma kinase (ALK)	Cancer
dALK-3 is an anaplastic lymphoma kinase (ALK) degrader. dALK-3 can effectively induce EML4-ALK degradation with a DC₅₀ of 0.182 μM. dALK-3 has good anti-proliferation activity against H3122 cells and can be used in the study of cancer .

HY-161750

PROTAC ALK degrader-2	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC₅₀ of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment .

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-155227

ALK/EGFR-IN-1	Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC₅₀ of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .

HY-163807

22-SLF	PROTACs FKBP	Cancer
22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC₅₀ of 0.5 µM in a FBXO22 dependent manner. 22-SLF degrades other endogenous proteins, such as *BRD4* and EML4-ALK fusion protein.(Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-163821); Blue: Ligand for E3 ligase (HY-163826)) .

HY-143557

Trk-IN-7	Trk Receptor	Cancer
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC₅₀s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC₅₀<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC₅₀=5-50 nM) .

HY-12215

Lorlatinib 30+ Cited Publications PF-06463922	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-135509

Lorlatinib acetate PF-06463922 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-12215R

Lorlatinib (Standard) PF-06463922 (Standard)	Reference Standards Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK ^L1196), 14-80 nM (ALK ^G1269A), 38-50 nM (ALK ^1151Tins), 77-113 nM (ALK ^G1202R), respectively .

HY-155227B

ALK/EGFR-IN-3	Anaplastic lymphoma kinase (ALK)	Cancer
ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.1360, 0.0332, and 0.0339 μM, respectively .

HY-131244

ALK-IN-9	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC₅₀s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .

HY-155227A

ALK/EGFR-IN-2	Anaplastic lymphoma kinase (ALK)	Cancer
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.0034, 0.0065, and 0.0018 μM, respectively .

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 .

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EML4-ALK

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