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 hydrochloride

CAS No. :

MCE 国际站：Zelavespib hydrochloride

产品活性：Zelavespib (PU-H71) hydrochloride 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 hydrochloride 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 hydrochloride (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最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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。