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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
40 Results for "
lymphoma xenograft models
" in MedChemExpress (MCE) Product Catalog:
Products (40)
40 Results for "lymphoma xenograft models" in MCE Product Catalog:
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10 Publications Verification
Synonyms: LOXO-305
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
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Tolinapant (ASTX660) is an orally active cIAP1/2 and XIAP antagonist, with an IC50 of < 40 nM against XIAP and an IC50 of <12 nM against cIAP1. Tolinapant triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant inhibits tumor growth in mouse xenograft models. Tolinapant can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors .
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Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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1 Cited Publications
Cat. No.: HY-P99272
CAS No.: 1375830-34-4
Synonyms: BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
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1 Cited Publications
MS-L6 is a OXPHOS inhibitor and antimalarial agent. MS-L6 inhibits NADH oxidation and electron transport. MS-L6 induces OXPHOS uncoupling, dissipates mitochondrial membrane potential, increases non-ATP-coupled oxygen consumption, and reduces ATP synthesis. MS-L6 triggers the production of ROS. MS-L6 exhibits anti-amoebic activity. MS-L6 exerts antitumor activity in mouse lymphoma xenograft models. MS-L6 can be used in research related to B-cell lymphoma, T-cell lymphoma, and non-Hodgkin B-cell lymphoma .
NRX-0492 is an orally active BTK PROTAC degrader, with a binding IC50 of 1.2 nM for both wild-type BTK and BTK T474I, and 2.7 nM for BTK C481S, and exhibits cellular DC50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTK C481S, respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK, inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-160698
CAS No.: 2661481-41-8
Synonyms: SGR-1505
SGR-1505 is an oral small molecule MALT1 inhibitor with anti-proliferative and antitumor activity.SGR-1505 inhibits MALT1 enzymatic activity to modulate NF-κB pathway gene expression.SGR-1505 induces modulation of cell cycle, DNA damage, and apoptosis-related genes in in vivo tumor samples.SGR-1505 exerts tumorostatic and regressive activity in ABC-DLBCL xenograft models.SGR-1505 can be used for the research of activated B cell-like diffuse large B cell lymphoma, non-Hodgkin B-cell lymphomas, chronic lymphocytic leukemia, and mature B cell neoplasms .
CCT374705 is an orally active BCL6 inhibitor (IC50 = 4.8 nM) with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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CCT373566 is an orally active BCL6 Molecular glue degrader with a DC50 of 0.7 nM. CCT373566 induces proteasomal degradation of BCL6 by promoting the formation of higher-order BCL6 complexes recognizable by E3 ligases. CCT373566 reduces tumor growth in lymphoma xenograft models. CCT373566 can be used in research related to diffuse large B-cell lymphoma .
Cat. No.: HY-P99922
CAS No.: 2173096-82-5
Cat. No.: HY-119715
CAS No.: 486414-35-1
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AG-012986 is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .
Cat. No.: HY-163962
CAS No.: 2451070-32-7
Target:
PROTACs Btk Bcr-Abl Toll-like Receptor (TLR) Fc Receptor (FcR) NOD-like Receptor (NLR) PERK p38 MAPK NF-κB TNF Receptor
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L18I is a Bruton's tyrosine kinase (BTK) PROTAC degrader that targets wild-type and BTK C481, and recruits the cereblon E3 ligase to mediate proteasomal degradation. L18I regulates the BCR, TLR, FcγR and NLRP3 inflammasome signaling pathways, inhibits the phosphorylation of PLCγ-2, ERK1/2 and p38, and reduces the levels of B cell activation markers CD25, CD69 and CD86. L18I downregulates the NF-κB, TNF and TLR signaling pathways, reduces the production of pro-inflammatory cytokines, and decreases immune cell infiltration and immune complex deposition. L18I inhibits the proliferation of BTK-expressing lymphoma cells, induces tumor regression in xenograft models, and exhibits synergistic activity when combined with inhibitors of SYK, PI3K or Lyn. L18I can be used in research related to lupus, diffuse alveolar hemorrhage and B-cell lymphoma .
Cat. No.: HY-P991057
CAS No.: 2376730-61-7
Cat. No.: HY-161989
CAS No.: 3105664-95-4
DZ-837 is a BCL6 PROTAC degrader with a DC50 of 557.7 nM. DZ-837 induces BCL6 ubiquitination and degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. DZ-837 activates CDKN1A and CDKN1B, the downstream genes of BCL6. DZ-837 upregulates p21 and p27 proteins . DZ-837 inhibits tumor growth in a diffuse large B-cell lymphoma xenograft mouse model. DZ-837 exerts synergistic antiproliferative effects when combined with Ibrutinib (HY-10997). DZ-837 can be used in studies related to diffuse large B-cell lymphoma .
Cat. No.: HY-156566
CAS No.: 2503036-46-0
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PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
Cat. No.: HY-177750
CAS No.: 2417647-40-4
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TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
Cat. No.: HY-175342
CAS No.: 2248046-39-9
Synonyms: LOXO-338
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FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .
Cat. No.: HY-156249
CAS No.: 1466546-45-1
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NMS-P528 is a DNA minor groove alkylating agent and ADC payload. NMS-P528 undergoes intramolecular cyclization to form reactive electrophilic derivatives, which in turn induce DNA damage, cell cycle arrest, and Apoptosis. NMS-P528 shows no significant anti-tumor activity as a free payload in a HER2-negative Raji lymphoma mouse xenograft model. NMS-P528 serves as the cytotoxic payload for the antibody-drug conjugate EV20/NMS-P945. NMS-P528 can be used in research related to breast cancer, gastric cancer, colon adenocarcinoma, Burkitt's lymphoma, neuroblastoma, pancreatic cancer, prostate cancer, head and neck cancer, ovarian cancer, and melanoma .
Cat. No.: HY-178777
CAS No.: 3084696-50-1
BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
Cat. No.: HY-156292
CAS No.: 3018914-66-1
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IHMT-EZH2-426 is an orally active and selective EZH2 degrader. IHMT-EZH2-426 forms a covalent bond with Cys663 of EZH2, inhibits its catalytic activity, and reduces the protein levels of EZH2 as well as the level of H3K27me3. IHMT-EZH2-426 acts as an antiproliferative agent against B-cell lymphoma and triple-negative breast cancer cells, and also exhibits anti-tumor related activity in Pfeiffer and MDA‑MB‑231 xenograft models. IHMT-EZH2-426 can be used in studies related to B-cell lymphoma and triple-negative breast 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
