Dimethyl Sulfoxide
Apexbio Technology LLC Tivozanib (AV-951) 475108-18-0 10mM (in 1mL DMSO)
Tivozanib (AV-951 CAS 475108-18-0) is a quinoline-urea derivative functioning as a potent inhibitor of vascular endothelial growth factor receptors (VEGFR) It primarily targets VEGFR-2 kinase demonstrating significant inhibitory activity in picomolar ranges (IC50 of approximately 160 pM) Additionally Tivozanib displays considerable selectivity causing minimal off-target interaction with c-kit In cellular assays it inhibits PDGFR and c-kit phosphorylation at nanomolar levels Preclinical evaluations revealed antitumor activity across multiple solid tumor xenograft models particularly renal cell carcinoma (RCC) Its mechanism and selectivity profile render it valuable for cancer research clinical investigation and preclinical efficacy assessments
Apexbio Technology LLC LY2157299(Synonyms: Galunisertib, LY-2157299, LY2157299 monohydrate, LY2157299 hydrate, LY2157299 free base), 10mM (in 1mL DMSO), CAS: 700874-72-2.
LY2157299 (CAS 700874-72-2) is a small-molecule antagonist that selectively targets the transforming growth factor-beta type I receptor (T RI) By blocking signaling through T RI it prevents phosphorylation of downstream effectors Smad2 and Smad3 thereby interfering with the TGF- signaling pathway Preclinical studies indicate LY2157299 inhibits 1-integrin activation reduces tumor cell invasion lowers connective tissue growth factor (CTGF) production and suppresses angiogenesis Currently in phase II clinical trials LY2157299 is being investigated primarily for therapeutic potential against hepatocellular carcinoma and glioblastoma
Apexbio Technology LLC THZ1 1604810-83-4 10mM (in 1mL DMSO)
THZ1 (CAS 1604810-83-4) is a covalent inhibitor of cyclin-dependent kinase 7 (CDK7) targeting specifically the cysteine residue C312 outside its kinase domain It exhibits potent inhibition with an IC50 of 3 2 nM against CDK7 in kinase binding assays In cellular studies THZ1 suppresses proliferation of Jurkat and Loucy T-cell acute lymphoblastic leukemia (T-ALL) cell lines (IC50 50 nM and 0 55 nM respectively) by disrupting CDK7-mediated signaling transcriptional regulation mediated by RUNX1 and RNA polymerase II CTD phosphorylation Thus THZ1 is utilized in cancer research to investigate transcriptional dysregulation in malignancies
Apexbio Technology LLC GSK1904529A 1089283-49-7 10mM (in 1mL DMSO)
GSK1904529A (CAS 1089283-49-7) is a small-molecule inhibitor targeting insulin-like growth factor-I receptor (IGF-1R) Mechanistically it acts as a reversible ATP-competitive antagonist inhibiting IGF-1R kinase activity with an IC50 of approximately 27 nM and a Ki value of 1 6 nM In NIH-3T3/LISN cells it reduces IGF-1R phosphorylation at an IC50 of about 22 nM subsequently attenuating phosphorylation of downstream effectors such as AKT IRS-1 and ERK pathways GSK1904529A also suppresses proliferation in various tumor cell lines through cell-cycle arrest at the G1 phase and demonstrates tumor growth inhibition in xenograft mouse models It serves as a research tool for investigating IGF-1R signaling in oncology
Apexbio Technology LLC Dinaciclib (SCH727965)(Synonyms: SCH-727965, SCH727965, Dinaciclib, MK-7965, MK7965), 10mM (in 1mL DMSO), CAS: 779353-01-4.
Dinaciclib (SCH727965 CAS 779353-01-4) is a small-molecule inhibitor targeting cyclin-dependent kinases (CDKs) specifically CDK1 CDK2 CDK5 and CDK9 It exhibits inhibitory potencies with IC50 values of 3 nM for CDK1 1 nM for CDK2 and CDK5 and 4 nM for CDK9 By suppressing CDK activity dinaciclib interrupts cell cycle progression reduces phosphorylation of retinoblastoma (Rb) protein and triggers apoptosis In addition dinaciclib interacts with the acetyl-lysine binding regions within bromodomains Currently in clinical phases I/II it demonstrates antitumor activity both in vitro and in animal models highlighting its potential applicability in oncology research
Apexbio Technology LLC Cinobufagin 470-37-1 10mM (in 1mL DMSO)
Cinobufagin (CAS 470-37-1) is a steroidal cardiac glycoside recognized for its inhibitory effect on the Na /K -ATPase pump Its inhibitory potency is approximately comparable to that of ouabain By impeding Na /K -ATPase activity cinobufagin disrupts ionic gradients altering intracellular calcium homeostasis and influencing cardiac and cellular functions In biomedical research cinobufagin serves as a valuable pharmacological tool to investigate ion transport mechanisms and explore related signaling pathways implicated in cellular physiology and pathology
Apexbio Technology LLC Temsirolimus 162635-04-3 10mM (in 1mL DMSO)
Temsirolimus (CCI-779) is an ester analog of rapamycin functioning as an inhibitor of the mammalian target of rapamycin (mTOR) The compound suppresses mTOR signaling pathways thus inhibiting cellular proliferation and growth In preclinical studies on breast cancer cell lines Temsirolimus displayed inhibitory activities with reported IC50 values of 0 6 nM in BT-474 cells 0 7 nM in MDA-MB-468 and SKBR-3 cells and 50 nM in MCF-7 cells It has been examined in xenograft models of tumors with PTEN mutations and multiple myeloma for investigating pathways related to cell-cycle progression and proliferation regulated by mTOR
Apexbio Technology LLC Fruquintinib(HMPL-013) 1194506-26-7 10mM (in 1mL DMSO)
Fruquintinib (HMPL-013 CAS 1194506-26-7) is a small molecule inhibitor targeting VEGFR family receptor tyrosine kinases (VEGFR1 VEGFR2 and VEGFR3) It demonstrates potent inhibitory activity with reported IC50 values of approximately 33 nM (VEGFR1) 35 nM (VEGFR2) and 0 5 nM (VEGFR3) Kinase selectivity screening indicates limited off-target effects against other kinases such as RET FGFR-1 and c-kit In preclinical tumor xenograft studies (e g gastric cancer BGC-823 model) significant tumor growth suppression ( 80%) was achieved at sustained therapeutic exposure Fruquintinib is currently under clinical investigation for cancer treatment based on its selective VEGFR pathway inhibition
Apexbio Technology LLC SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation
Apexbio Technology LLC GDC-0032 1282512-48-4 10mM (in 1mL DMSO)
GDC-0032 (CAS 1282512-48-4) is a benzofused small-molecule inhibitor targeting PI3K with high potency and selectivity It demonstrates strong inhibitory activity against PI3K PI3K and PI3K with IC50 values of 0 29 nM 0 91 nM and 0 97 nM respectively and notably exhibits greater selectivity towards PI3K In vitro GDC-0032 effectively inhibits cell proliferation and cellular function showing EC50 values of 25 nM (MCF7 cells) and 571 nM (PC3 cells) with corresponding IC50 values of 4 nM and 31 nM In vivo experiments indicate antitumor activity in MCF7-neo/Her2 xenograft models GDC-0032 serves as a valuable tool compound for PI3K-related oncology research
Apexbio Technology LLC Bexarotene 153559-49-0 10mM (in 1mL DMSO)
Bexarotene is a synthetic selective agonist for retinoid X receptors (RXRs) a subclass of nuclear hormone receptors involved in the regulation of gene transcription Upon binding to RXRs Bexarotene modulates the expression of target genes associated with cell differentiation proliferation and apoptosis Due to this mechanism Bexarotene is commonly employed in research investigating tumor growth inhibition cellular differentiation pathways and apoptosis induction Researchers also frequently utilize this retinoid derivative to elucidate RXR-mediated signaling pathways in oncology and to explore potential therapeutic applications for various malignancies
Apexbio Technology LLC Ezetimibe 163222-33-1 10mM (in 1mL DMSO)
Ezetimibe (CAS 163222-33-1) is a cholesterol absorption inhibitor that targets the intestinal cholesterol transporter Niemann-Pick C1 Like 1 (NPC1L1) It reduces intestinal uptake of cholesterol and dietary carotenoids including - and -carotene lycopene lutein and -cryptoxanthin through downregulating transport proteins such as SR-BI ABCA1 NPC1L1 and transcription factors including SREBP-1/-2 and LXR- In ApoE-deficient mouse models ezetimibe significantly decreases plasma cholesterol levels and attenuates atherosclerotic lesion formation Clinically it lowers LDL cholesterol total cholesterol and triglycerides while elevating HDL cholesterol
Apexbio Technology LLC Busulfan 55-98-1 10mM (in 1mL DMSO)
Busulfan is a DNA alkylating agent widely used in biomedical research as an anticancer compound It functions by forming cross-links on guanine bases within DNA leading to DNA damage and subsequent inhibition of cell growth and proliferation In vitro studies reveal that exposure to busulfan (IC50 range approximately 7 5 120 M) promotes cellular senescence in normal human fibroblast cell lines mediated through increased reactive oxygen species (ROS) and sustained activation of MAPK signaling pathways Additionally busulfan is utilized in fertility and reproductive biology research due to its ability to induce apoptosis in male germ cells reducing germ cell populations in experimental mouse models
Apexbio Technology LLC CGP 57380 522629-08-9 10mM (in 1mL DMSO)
CGP 57380 (CAS 522629-08-9) is a specific and selective inhibitor targeting the serine/threonine kinase MNK1 an enzyme implicated in translation regulation via phosphorylation of the eukaryotic initiation factor 4E (eIF4E) It inhibits MNK1 activity in vitro with an IC50 of approximately 2 2 M CGP 57380 suppresses stimulus-induced phosphorylation of eIF4E in various cellular contexts including 293 cells vascular smooth muscle cells and macrophages reducing translation of mRNAs encoding proinflammatory mediators such as TNF- IL-6 and monocyte chemoattractant protein-1 (MCP-1) Hence CGP 57380 is valuable for investigating MNK1-mediated translational control in inflammation and cell signaling
Apexbio Technology LLC BYL-719 1217486-61-7 10mM (in 1mL DMSO)
BYL-719 (CAS 1217486-61-7) is a selective inhibitor of PI3K demonstrating minimal activity against PI3K or isoforms Through targeting PI3K an essential node frequently dysregulated via PIK3CA mutations in various cancers BYL-719 effectively disrupts downstream proliferative signaling In biochemical assays BYL-719 shows potent inhibition of PI3K with an IC50 of 5 nM Preclinical evaluations indicate dose-dependent antitumor efficacy in xenograft tumor models and proliferation arrest and apoptosis induction in multiple myeloma cell lines exhibiting PIK3CA overexpression Clinically initial studies reveal manageable safety profiles and preliminary antitumor responses notably in PIK3CA-mutant malignancies supporting continued exploration in oncology research settings