MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Zelavespib

CAS No. : 873436-91-0

MCE 站：Zelavespib

产品活性：Zelavespib (PU-H71) 是一种有效的 Hsp90 抑制剂，在 MDA-MB-468 细胞中，对 Hsp90 的 IC₅₀ 值为 51 nM。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease

作用靶点：HSP

In Vitro: Zelavespib is a potent Hsp90 inhibitor, with an IC₅₀ of 51 nM in MDA-MB-468 cells. Zelavespib inhibits the growth of several tumor cells, such as MDA-MB-468, MDA-MB-231 ａnd HCC-1806 cells, with IC₅₀s of 65 ± 8 nM, 140 ± 5 nM ａnd 87 ± 3 nM, respectively, ａnd such inhibition is associated with a G2-M block arrest. Zelavespib (10-1000 nM) induces significant apoptosis in triple-negative breast cancers (TNBCs). Zelavespib (0.5, 1 μM) also downregulates oncoproteins involved in the invasive potential of TNBCs. Zelavespib (0.5 μM) decreases ａnd depletes the BCR signaling kinases. Zelavespib (0.25-10 μM) is cytotoxic to CLL cells but shows minimal effects on PBMC or resting B cells. In addition, Zelavespib (0-1μM) reduces CLL viability via the induction of mitochondrial apoptosis, ａnd antagonizes the survival signals from CLL microenvironment at 0.5 μM. Zelavespib (0.05 μM) induces apoptosis of MDA-MB-231, BT-474, ａnd MCF7 cells, ａnd such induction is enhanced by TNF-α. Zelavespib (0.05 μM) degradates IKKβ, ａnd down-regulates the NF-κB transcriptional activity induced by TNF-α treatment.

In Vivo: Zelavespib (75 mg/kg, i.p.) causes intratumor accumulation, extends down-regulation of anti-tumor driving molecules, completes ａnd retains responses at nontoxic doses in MDA-MB-468 tumor-bearing mice. Zelavespib(75 mg/kg 3×week, i.p.) suppresses the gowth of tumors, ａnd such an effect is associated with down-regulation of several Hsp90-regulated malignancy driving proteins.

相关产品：Hsp90-IN-17  |  KNK423  |  Palmitic acid  |  HSP90-IN-18  |  Paeoniflorin  |  Pimitespib  |  Debio 0932  |  HSP90-IN-22  |  KU-177  |  AMP-PCP disodium  |  Tamoxifen  |  JG-231  |  MPC-0767  |  SNX-2112  |  HDAC6/HSP90-IN-1  |  TRC051384 hydrochloride  |  Retaspimycin  |  Onalespib  |  HM03  |  EC144  |  MAO A/HSP90-IN-1  |  2-Hexyl-4-pentynoic acid  |  Cucurbitacin D  |  Shepherdin (79-87) (TFA)  |  NCT-58  |  MKT-077  |  Cemdomespib  |  6BrCaQ-C10-TPP

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿*全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。