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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
23 Results for "
H3122
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "H3122" in MCE Product Catalog:
2
2 Cited Publications
Research Areas:
TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984) .
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TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984) .
Cat. No.: HY-164397
CAS No.: 3117862-69-5
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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 .
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-175527
Research Areas:
ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
Cat. No.: HY-172426
CAS No.: 1893419-37-8
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Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50% .
Cat. No.: HY-170592
Target:
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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 .
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-161750
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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-120663
CAS No.: 1884321-89-4
Target:
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KRCA-0713 is an ALK inhibitor with anti-ALK activity. KRCA-0713 showed promising anti-ALK activity in enzyme and cell-based experiments. KRCA-0713 was shown to effectively inhibit ALK-driven tumor growth in H3122 xenograft model studies, similar to the effect of ceritinib .
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-175849
Research Areas:
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-180966
CAS No.: 3057939-66-6
Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .
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 .
Cat. No.: HY-179732
PROTAC ALK degrader-4 (Compound B8) is an ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 exhibits excellent anti-proliferative activity against NCI-H2228 and NCI-H3122. PROTAC ALK degrader-4 leads to a significant downregulation of 390 proteins, including IGF-1R and its downstream proteins such as ERK1/2 and STAT3. PROTAC ALK degrader-4 can be used for research on lung adenocarcinoma .
Cat. No.: HY-180964
CAS No.: 3057939-67-7
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Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research .
Cat. No.: HY-180956
CAS No.: 2379672-57-6
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PROTAC ALK degrader-5 (Compound 17) is an efficient ALK PROTAC degrader, with its inhibitory effects on EML4-ALK and NPM-ALK being 27.4 nM and 116.5 nM respectively. PROTAC ALK degrader-5 exhibits potent anti-proliferative activity against H3122 and Karpas 299. PROTAC ALK degrader-5 effectively inhibits the phosphorylation of ALK and STAT3. PROTAC ALK degrader-5 can be used for the study of ALK-driven malignant tumors, such as human non-small cell lung cancer and anaplastic large cell lymphoma .
Cat. No.: HY-151155
CAS No.: 3033549-18-4
Target:
Research Areas:
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-180965
CAS No.: 3057939-64-4
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Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
Cat. No.: HY-180972
CAS No.: 2417174-28-6
Research Areas:
PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research .
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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
