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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
G1202R
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "G1202R" in MCE Product Catalog:
38
38 Publications Verification
Synonyms: PF-06463922
Research Areas:
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis 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 .
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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 .
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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 .
Cat. No.: HY-12215R
CAS No.: 1454846-35-5
Synonyms: PF-06463922 (Standard)
Research Areas:
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 Kis 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 .
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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.
Cat. No.: HY-E70645
Target:
Research Areas:
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 .
Research Areas:
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 .
Cat. No.: HY-147219A
Purity: 99.84%
SIAIS164018 hydrochloride is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 hydrochloride promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 hydrochloride induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 hydrochloride exhibits preferential inhibitory activity against FER kinase. SIAIS164018 hydrochloride can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer .
Research Areas:
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 .
Cat. No.: HY-135509
CAS No.: 1924207-18-0
Synonyms: PF-06463922 acetate
Research Areas:
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis 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 .
Cat. No.: HY-147219
CAS No.: 2353492-68-7
SIAIS164018 is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 exhibits preferential inhibitory activity against FER kinase. SIAIS164018 can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer .
Cat. No.: HY-146408
CAS No.: 2901889-01-6
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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 .
Cat. No.: HY-174314
CAS No.: 2845188-22-7
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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 .
Cat. No.: HY-105369
CAS No.: 154015-73-3
Research Areas:
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 .
Cat. No.: HY-174315
Research Areas:
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)
Cat. No.: HY-146022
CAS No.: 2353494-84-3
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SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors .
Cat. No.: HY-157391
Research Areas:
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 .
Cat. No.: HY-147833
CAS No.: 2468219-09-0
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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 .
Cat. No.: HY-151155
CAS No.: 3033549-18-4
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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 .
Cat. No.: HY-143557
CAS No.: 2383011-61-6
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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) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
