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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
46 Results for "
ALK PROTAC
" in MedChemExpress (MCE) Product Catalog:
Products (46)
46 Results for "ALK PROTAC" in MCE Product Catalog:
4
4 Cited Publications
Research Areas:
MS4078 is a ALK PROTAC degrader with a DC50 of 11 nM in SU-DHL-1 cells and a DC50 of 59 nM in NCI-H2228 cells, and its Kd value for ALK binding is 19 nM. MS4078 induces ALK degradation via the ubiquitin-proteasome pathway by recruiting cereblon, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4078 is applicable for the research of non-small cell lung cancer and anaplastic large cell non-Hodgkin's lymphoma .
3
Target:
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Alkynyl Palmitic Acid (Alk-C16) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs . Alkynyl Palmitic Acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2
2 Cited Publications
TL13-112 is a ALK PROTAC degrader. TL13-112 degrades the NPM-ALK protein by recruiting the CRBN E3 ligase, thereby blocking oncogenic signal transduction such as STAT3, ERK and AKT, and relieving the transcriptional repression of CD45, CCR7 and PI3Kδ. TL13-112 can be used in related research on anaplastic large cell lymphoma .
Research Areas:
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 .
Research Areas:
TL13-12 is a CRBN-recruiting ALK PROTAC degrader, with a DC50 of 10 nM in H3122 cells. TL13-12 induces dimerization of CRBN and truncated ALK, which brings the DNA-binding domain and transactivation domain into close proximity, thereby activating the expression of downstream reporter genes, while exhibiting extremely low leaky expression under non-inducing conditions. TL13-12 serves as a tool molecule for the orthogonal PROTAC-CID system, and is applied in research on non-small cell lung cancer, anaplastic large cell lymphoma, and neuroblastoma .
Cat. No.: HY-171825
CAS No.: 2570251-63-5
Research Areas:
SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC50 of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas .
Cat. No.: HY-174368
Synonyms: Pro-BA
Research Areas:
PROTAC EML4-ALK Degrader-1 (Pro-BA) is an orally active EML4-ALK PROTAC degrader that recruits GID4, with a Kd value of 144 nM against human EML4-ALK and a DC50 of 74 nM in H3122 cells. PROTAC EML4-ALK Degrader-1 promotes EML4-ALK ubiquitination and proteasomal degradation, reduces cancer cell viability, inhibits cancer cell and tumor growth, induces apoptosis, and alters cell cycle distribution. PROTAC EML4-ALK Degrader-1 can be used in studies related to EML4-ALK-positive cancers and non-small cell lung cancer .
Cat. No.: HY-159147
CAS No.: 2570251-69-1
Target:
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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) .
Research Areas:
Brigatinib C is a prodrug of ALK inhibitor, which can be used to syntheis PROTACs .
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 .
Cat. No.: HY-170405
CAS No.: 2940242-88-4
Research Areas:
YB-3-17 is a blood-brain barrier permeable mTOR inhibitor (IC50 = 0.22 nM) and GSPT1 PROTAC degrader. YB-3-17 inhibits mTORC1/2, CK1δ/ε, mutant ALK and HER2 kinases, induces CRBN-dependent selective GSPT1 degradation, ablates mTOR downstream phosphorylation, downregulates c-Myc/Cyclin D1 to impair tumor translation, triggers p53-mediated apoptosis, suppresses tumor proliferation and xenograft tumor growth, and can be used for the study of glioma, neuroblastoma, breast cancer, lymphoma, colorectal cancer and lung cancer .
Cat. No.: HY-W754809
CAS No.: 2353496-79-2
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ALK ligand-1 is a ALK ligand that can be used for synthesis of PROTAC ALK degrader-4 (HY-175527) .
Cat. No.: HY-161749
CAS No.: 3049802-45-8
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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 .
Cat. No.: HY-169481
CAS No.: 3027918-96-0
Research Areas:
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-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-168551
Research Areas:
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-174315
Research Areas:
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-161750
Research Areas:
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 .
Cat. No.: HY-174314
CAS No.: 2845188-22-7
Research Areas:
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-177945
CAS No.: 3055593-63-7
Synonyms: Gal-MS99
Research Areas:
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 .
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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
