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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
39 Results for "
lung tumor regression
" in MedChemExpress (MCE) Product Catalog:
Products (39)
39 Results for "lung tumor regression" in MCE Product Catalog:
32
32 Publications Verification
Synonyms: VS-6062
PF-562271 (VS-6062) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma .
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32 Publications Verification
Synonyms: VS-6062 (besylate)
PF-562271 besylate (VS-6062 besylate) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 besylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 besylate exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 besylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 besylate can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma .
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PF-562271 hydrochloride (VS-6062 hydrochloride) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 hydrochloride induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 hydrochloride exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 hydrochloride reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 hydrochloride can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma .
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Indisulam (E 7070) is a carbonic anhydrase inhibitor and RBM39 molecular glue degrader, with Ki values of 31, 15, and 24 nM against human carbonic anhydrase I, II, and IX, respectively, and a Ki value of 65 nM against bovine carbonic anhydrase IV. Indisulam promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase complex, triggering polyubiquitination and proteasomal degradation of RBM39. Indisulam induces aberrant pre-mRNA splicing, G1 cell cycle arrest, and cell death in cancer cells. As an anticancer agent, Indisulam drives tumor regression and growth inhibition in xenograft models. Indisulam can be used in research related to solid tumors, hematologic and lymphoid malignancies, colorectal cancer, and non-small cell lung cancer .
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1 Cited Publications
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
Cat. No.: HY-175749
CAS No.: 3025467-07-3
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BMS-986463, a CRBN E3 ligase modulator (CELMoD), is a WEE1 kinase molecular glue degrader. BMS-986463 significantly inhibits tumor regression and reduces the level of phospho-CDK2. BMS-986463 can be used for advanced malignant solid tumors like non-small cell lung cancer (NSCLC) research .
Cat. No.: HY-159607
CAS No.: 2755761-78-3
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PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
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QCA570 is a pan-BET-BRD PROTAC degrader. QCA570 degrades BRD2/3/4 and BRDT via cereblon and the ubiquitin-proteasome pathway, inhibits the expression of c-MYC, EZH2 and Mcl-1, induces tumor cell apoptosis, cycle arrest and regression, and exerts a synergistic inhibitory effect on Osimertinib (HY-15772)-resistant EGFR-mutant non-small cell lung cancer. QCA570 can be used in the research of acute myeloid leukemia, acute lymphoblastic leukemia, bladder cancer and non-small cell lung cancer .
Cat. No.: HY-172429
CAS No.: 2489185-38-6
Synonyms: ORIC-114
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Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-172429A
Synonyms: ORIC-114 hemihydrate
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Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-175870
CAS No.: 3024878-19-8
Eras-4001 is a potent, orally active pan-KRAS inhibitor with Kd values of 110, 13 and 39 pM against wild-type, G12D and G12V mutant KRAS, respectively, and exhibits selectivity toward wild-type HRAS and NRAS. Eras-4001 inhibits ERK1/2 phosphorylation and cell viability in cancer cells. Eras-4001 induces tumor growth inhibition and regression in subcutaneous xenograft models. Eras-4001 can be used in research on non-small cell lung cancer, ovarian cancer, etc.
Cat. No.: HY-148511
CAS No.: 147063-80-7
Synonyms: CMP-001
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Vidutolimod (CMP-001) is a virus-like particle containing a TLR9 activator . Vidutolimod induces human peripheral blood mononuclear cells to secrete IFNα, and upregulates the gene expression of CXCL10, PDL1, IDO and CD80. Vidutolimod activates TLR9, which in turn triggers plasmacytoid dendritic cell activation, production of IFNγ and TNFα, induction of CXCL10, and recruitment of antitumor T cells. Vidutolimod causes influenza-like symptoms, hypotension and tumor regression, and its activity depends on the presence of anti-Qβ antibodies. Vidutolimod modulates monocyte function, promotes CD4 T cell proliferation, and activates multiple immune cell types in an environment with anti-Qβ antibodies. Vidutolimod prolongs the survival of tumor-bearing mice. Vidutolimod is used in research related to advanced melanoma, head and neck squamous cell carcinoma, and advanced non-small cell lung cancer .
Cat. No.: HY-153974
CAS No.: 2254805-44-0
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BBT-176 is an orally active EGFR tyrosine kinase inhibitor. BBT-176 is a reversible ATP-competitive inhibitor with a unique binding mode, and it exhibits selectivity for mutant EGFR over wild-type EGFR. BBT-176 inhibits tumor growth, induces tumor regression, upregulates EGFR expression, and does not trigger secondary EGFR gene mutations. BBT-176 can be used in research related to non-small cell lung cancer .
Cat. No.: HY-178238
CAS No.: 3040077-52-6
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LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer .
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XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
Cat. No.: HY-164429
CAS No.: 2418533-90-9
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
Cat. No.: HY-178008
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Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
Cat. No.: HY-13650R
CAS No.: 165668-41-7
Synonyms: E 7070 (Standard)
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Indisulam (Standard) (E 7070 (Standard)) is the analytical standard of Indisulam (HY-13650). This product is intended for research and analytical applications. Indisulam (E 7070) is a carbonic anhydrase inhibitor and RBM39 molecular glue degrader, with Ki values of 31, 15, and 24 nM against human carbonic anhydrase I, II, and IX, respectively, and a Ki value of 65 nM against bovine carbonic anhydrase IV. Indisulam promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase complex, triggering polyubiquitination and proteasomal degradation of RBM39. Indisulam induces aberrant pre-mRNA splicing, G1 cell cycle arrest, and cell death in cancer cells. As an anticancer agent, Indisulam drives tumor regression and growth inhibition in xenograft models. Indisulam can be used in research related to solid tumors, hematologic and lymphoid malignancies, colorectal cancer, and non-small cell lung cancer .
Cat. No.: HY-132031
CAS No.: 2682939-53-1
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Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 is a drug-linker conjugate composed of a cleavable Val-Ala linker and the potent ADC cytotoxin PNU-159682 (HY-16700), which is applicable for ADC synthesis. When conjugated with an anti-CD46 antibody, Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 delivers its payload to CD46-expressing cells, while cathepsin B cleaves the Val-Ala linker to release the payload. ADCs synthesized from Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 drive durable responses in CD46-expressing patient-derived xenograft models of non-small cell lung cancer and colorectal cancer, and a single administration induces complete tumor regression in most models. Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 can be used in the research of non-small cell lung cancer and colorectal 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
