Dimethyl Sulfoxide
Apexbio Technology LLC Cediranib (AZD217) 288383-20-0 10mM (in 1mL DMSO)
Cediranib (AZD2171 CAS 288383-20-0) is an orally bioavailable small molecule inhibitor targeting the kinase insert domain receptor (KDR VEGFR-2) with potent inhibition observed in recombinant assays (IC50 1 nM) Additionally cediranib suppresses related vascular endothelial growth factor receptors VEGFR-1 (Flt-1 IC50 5 nM) and VEGFR-3 (Flt-4 IC50 3 nM) It also blocks select platelet-derived growth factor receptors notably c-Kit PDGFR PDGFR and CSF-1R at nanomolar to sub-micromolar concentrations indicating multiple-kinase targeting capability Cediranib serves as a valuable research compound for studying tumor angiogenesis and kinase-driven oncogenic pathways
Apexbio Technology LLC Fosaprepitant(Synonyms: Fosaprepitant dimeglumine, Emend IV, L-758298, MK-0517, Fosaprepitant meglumine, Ivemend), 10mM (in 1mL DMSO), CAS: 172673-20-0.
Fosaprepitant (CAS 172673-20-0) also known as MK-0517 or L-758 298 is a selective neurokinin-1 (NK-1) receptor antagonist exerting its pharmacological effects primarily through its active metabolite aprepitant This antagonism blocks substance P-mediated biological effects including vomiting responses In established preclinical models such as the cisplatin-triggered emesis in ferrets fosaprepitant demonstrated activity in mitigating chemotherapy-induced vomiting Given aprepitant s favorable penetration into the central nervous system fosaprepitant exhibits high NK-1 receptor affinity and potentiates antiemetic actions of agents such as dexamethasone and granisetron It is used in combination therapies with 5-HT3 antagonists and corticosteroids for chemotherapy-induced nausea and vomiting (CINV)
Apexbio Technology LLC PF-4708671 1255517-76-0 10mM (in 1mL DMSO)
PF-4708671 (CAS 1255517-76-0) is a cell-permeable small molecule that specifically inhibits p70 ribosomal S6 kinase 1 (S6K1) S6K1 regulates diverse cellular processes including protein synthesis and insulin signaling pathways PF-4708671 inhibits S6K1 with an IC50 of 160 nM in HEK293 cell-derived enzyme assays and has a reported Ki value of 20 nM in vitro It selectively inhibits S6K1 over structurally related kinases such as RSK2 and MSK1 hindering phosphorylation of downstream substrates including ribosomal protein S6 mTOR and Rictor PF-4708671 is valuable in biomedical research involving cancer and insulin resistance
Apexbio Technology LLC MLN2238(Synonyms: Ixazomib, MLN-2238, Ninlaro, MLN9708, Ixazomib citrate), 10mM (in 1mL DMSO), CAS: 1072833-77-2.
MLN2238 (CAS number 1072833-77-2) is a dipeptidyl boronic acid derivative designed as a reversible inhibitor of the 5 subunit (chymotrypsin-like activity) of the 20S proteasome with reported IC50 and Ki values of 3 4 nM and 0 93 nM respectively At higher concentrations MLN2238 also targets the proteasome s 1 (caspase-like) and 2 (trypsin-like) subunits In preclinical studies using xenograft and genetically-engineered models of hematologic malignancies MLN2238 exhibited potent antitumor activity promoting apoptosis and suppressing pathways such as NF- B MLN2238 has research applications in oncology particularly against multiple myeloma and lymphoma including in bortezomib-resistant cell lines
Apexbio Technology LLC Nilotinib(AMN-107) 641571-10-0 10mM (in 1mL DMSO)
Nilotinib (AMN-107 CAS 641571-10-0) is an orally bioavailable selective inhibitor targeting the BCR-ABL tyrosine kinase Derived structurally from imatinib nilotinib inhibits both wild-type (WT p210) and mutant forms (E281K E292K F317L M351T F486S) of BCR-ABL reducing their autophosphorylation activity with IC50 values ranging from 20 to 42 nM It also exhibits substantial inhibitory activity against activated KIT mutants (e g V560del K642E) and various KIT double mutations and effectively suppresses PDGFR and PDGFR kinases Nilotinib is utilized extensively in research related to chronic myeloid leukemia and gastrointestinal stromal tumors involving kinase-driven pathologies
Apexbio Technology LLC Celastrol 34157-83-0 10mM (in 1mL DMSO)
Celastrol (CAS 34157-83-0) is a triterpene compound isolated from the Chinese medicinal herb Thunder of God Vine It functions as a proteasome inhibitor targeting the proteolytic activities within the 20S and 26S proteasome complexes leading to intracellular accumulation of ubiquitinated substrates including I B- Bax and p27 thereby inducing apoptosis in cancer cell lines such as human prostate cancer (PC-3 and LNCaP) Celastrol also inhibits NF- B signaling decreasing LPS-induced production of inflammatory cytokines (TNF- and IL-1 ) in human PBMCs and augmenting TNF-mediated apoptosis in KBM-5 cells Its anti-inflammatory and pro-apoptotic properties make celastrol relevant in cancer and inflammation research
Apexbio Technology LLC UMI-77(Synonyms: UMI 77, UMI77, UMI-77 Mcl-1 inhibitor, Mcl-1 inhibitor UMI-77, 518303-20-3), 10mM (in 1mL DMSO), CAS: 518303-20-3.
UMI-77 (CAS 518303-20-3) is a small-molecule inhibitor targeting the anti-apoptotic protein Myeloid cell leukemia-1 (Mcl-1) a member of the Bcl-2 protein family implicated in apoptotic regulation and cell survival signaling Biochemical assays demonstrate that UMI-77 binds selectively to the BH3-binding groove of Mcl-1 protein competing effectively against pro-apoptotic BH3 peptides (Ki 0 49 M) Additionally UMI-77 disrupts the interaction of Mcl-1 with pro-apoptotic factors such as Bax (IC50 1 43 M) promoting apoptosis in cancer cells Preclinical studies on pancreatic cancer cell lines and BxPC-3 xenograft mouse models show that UMI-77 suppresses tumor growth and induces apoptotic cell death highlighting its value as a research tool for studying apoptosis-related oncogenic pathways