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Results for "

G1202R

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Anaplastic lymphoma kinase (ALK) (21) Apoptosis (9) Autophagy (1) EGFR (2) ERK (1) HDAC (1) Ligands for Target Protein for PROTAC (1) PROTACs (4) Reference Standards (1) ROS Kinase (5) Trk Receptor (1)
By Research Areas:	Cancer (21) Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12215

Lorlatinib Maximum Cited Publications 35 Publications Verification 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-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-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-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-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-E70645

*ALK G1202R* Recombinant Human Active Protein Kinase**	Anaplastic lymphoma kinase (ALK)	Cancer
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase in the insulin receptor superfamily. ALK can be used for the study of non-small cell lung carcinoma (NSCLC). ALK has multiple mutants. ALK G1202R Recombinant Human Active Protein Kinase is a recombinant ALK G1202R protein that can be used to study ALK G1202R-related functions .

HY-147219A

SIAIS164018 hydrochloride	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .

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-112801

F-1	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC₅₀s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK ^WT, ROS1 ^WT, ALK ^L1196M and ALK ^G1202R, respectively .

HY-147219

SIAIS164018	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .

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-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-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-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-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-157391

ALK/ROS1-IN-3	ROS Kinase Anaplastic lymphoma kinase (ALK)	Cancer
ALK/ROS1-IN-3 (compound C01) is a ROS1 and ALK dual inhibitor with IC₅₀s of 42.3 nM and 49.1 nM for ROS1 ^G2032R and ALK ^G1202R, respectively .

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-147833

ALK-IN-22	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC₅₀ values of 2.3, 3.7 and 2.9 nM for ALK, ALK ^L1196M and ALK ^G1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research .

HY-151155

ALK-IN-23	Anaplastic lymphoma kinase (ALK)	Cancer
ALK-IN-23 is a potent ALK inhibitor with IC₅₀ values of 1.6 nM, 0.71 nM and 1.3 nM for ALK ^WT, ALK ^L1196M and ALK ^G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .

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-180811

ALK/HDAC-IN-2	Anaplastic lymphoma kinase (ALK) HDAC Apoptosis	Neurological Disease
ALK/HDAC-IN-2 (Compound 19b) is an ALK/HDAC inhibitor with IC₅₀ values for ALK WT and total HDACs of 8 nM and 1.18 μM, respectively. ALK/HDAC-IN-2 exhibits inhibitory activity against ALK mutants *G1202R, F1174L, and L1196M, with IC₅₀* values of 2.74, 9.23, and 34.28 nM, respectively. ALK/HDAC-IN-2 shows potent and selective inhibition against HDAC1 (IC₅₀ = 0.24 μM), while its inhibitory activity against HDAC7, HDAC6, and HDAC11 is weak (IC₅₀ > 10 μM). ALK/HDAC-IN-2 has broad-spectrum anti-proliferative activity against various cancer cells, inducing cell cycle arrest and apoptosis. ALK/HDAC-IN-2 can be used for the study of neuroblastoma .

HY-116636

KRCA-0377	Anaplastic lymphoma kinase (ALK)	Cancer
KRCA-0377 is an orally active ALK inhibitor with an IC₅₀ of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer .

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G1202R

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