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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
21 Results for "
ALK fusions
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "ALK fusions" in MCE Product Catalog:
Synonyms: Brigatinib analog
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ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
Cat. No.: HY-P99752
CAS No.: 2315268-27-8
Synonyms: ALKS 4230; RDB-1450
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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 .
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MS4077 is an ALK PROTAC degrader with a DC50 of 3 nM in SU-DHL-1 cells, a DC50 of 34 nM in NCI-H2228 cells, and a Kd of 37 nM. MS4077 induces the degradation of oncogenic active ALK fusion proteins via a cereblon- and proteasome-dependent pathway, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4077 is used for the research of anaplastic large cell lymphoma and non-small cell lung cancer .
Cat. No.: HY-159147
CAS No.: 2570251-69-1
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
Cat. No.: HY-169481
CAS No.: 3027918-96-0
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AP-1 is a targeted ALK PROTAC degrader. AP-1 effectively degrades various ALK fusion/mutation forms, including degradation of NPM-ALK (DC50 = 4.6 nM) and EML4-ALK (DC50 = 357.6 nM), and exhibits a typical hook effect at high concentrations. AP-1 inhibits phosphorylation of downstream STAT3, downregulates gene expression in the JAK-STAT pathway, and kills ALK-positive tumor cells via activating the caspase-3-dependent apoptosis pathway. AP-1 shows cytotoxicity against a variety of cancer cells and possesses anti-tumor activity. AP-1 can be used in research related to non-small cell lung cancer, neuroblastoma, and anaplastic large cell lymphoma .
Cat. No.: HY-E70714
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EML4-ALK is a fusion-type protein tyrosine kinase produced through gene rearrangement. EML4-ALK can be used for the study of non-small cell lung carcinoma (NSCLC) and neuroblastoma (NB). EML4-ALK has multiple mutants. EML4 ALK F1174L Recombinant Human Active Protein Kinase is a recombinant EML4 ALK F1174L protein that can be used to study EML4 ALK F1174L-related functions .
Cat. No.: HY-174315
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WZH-17-002 is a CRBN‑recruiting ALK PROTAC degrader. WZH‑17‑002 degrades ALK proteins, including EML4‑ALK and the compound mutants. WZH‑17‑002 inhibits the development of drug resistance in ALK‑fusion non‑small‑cell lung cancer. WZH‑17‑002 can be used for research related to non‑small‑cell lung cancer .
Cat. No.: HY-172426
CAS No.: 1893419-37-8
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Dirozalkib is an orally active and blood-brain barrier-penetrant ALK tyrosine kinase inhibitor. Dirozalkib inhibits the proliferation of ALK fusion-positive and ALK TKI-resistant tumor cells, and inhibits tumor growth in PDX and intracranial xenograft lung cancer models. Dirozalkib can be used for research related to non-small cell lung cancer .
Cat. No.: HY-175849
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ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .
Cat. No.: HY-105369
CAS No.: 154015-73-3
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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-175271
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JWJ-01-378 is a TPM3-TRKA fusion protein inhibitor and a wild-type TRK PROTAC degrader. JWJ-01-378 induces degradation via the ubiquitin-proteasome system, and does not degrade TRK inhibitor-resistant mutants or ALK fusion proteins. JWJ-01-378 inhibits downstream signaling pathways activated by TPM3-TRKA fusion, and reduces the viability of cancer cells harboring TPM3-TRKA fusion. JWJ-01-378 can be used to evaluate targeted degradation of TRK fusion proteins in cancer .
Cat. No.: HY-177945
CAS No.: 3055593-63-7
Synonyms: Gal-MS99
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MS99-β-Gal (Gal-MS99) is a galactose-modified NPM-ALK PROTAC degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC50 of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC50 = 2.162 μM). MS99-β-Gal can be used for the research of cancer .
Cat. No.: HY-E70713
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EML4-ALK is a fusion-type protein tyrosine kinase produced through gene rearrangement. EML4-ALK is a potential molecular target in non-small cell lung carcinoma (NSCLC). EML4 ALK Recombinant Human Active Protein Kinase is a recombinant EML4 ALK protein that can be used to study EML4 ALK-related functions .
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-13464R
CAS No.: 1197958-12-5
Synonyms: Brigatinib analog (Standard)
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ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
Cat. No.: HY-168551
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PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC50 of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma) .
Cat. No.: HY-186338
CAS No.: 845812-90-0
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ALK-IN-39 is an ALK inhibitor. ALK-IN-39 targets anaplastic lymphoma kinase fusion proteins and inhibits NPM-ALK-dependent proliferation. ALK-IN-39 inhibits the proliferation of cells expressing Tel-InsR as well as wild-type hematopoietic cells and anaplastic large cell lymphoma cells. ALK-IN-39 can be used in research on anaplastic large cell lymphoma (ALCL) .
Cat. No.: HY-187801
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SH-CER-6 is a double-warhead C 2-COUPL derived from Ceritinib (HY-187801) that targets the EML4-ALK fusion protein complex and induces its degradation. SH-CER-6 simultaneously binds to structures near the ALK inhibitor-binding region and forms a covalent conjugate with a protein cysteine, thereby promoting ubiquitination and proteasome-dependent degradation of the EML4-ALK complex, which in turn inhibits the ALK signaling pathway. SH-CER-6 is useful for research related to ALK-positive non-small cell lung cancer .
Cat. No.: HY-180970
CAS No.: 2162120-55-8
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TD-004 is a potent ALK PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC50 of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC50s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer .
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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
