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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 747412-49-3 |
| 是否进口 | 否 |
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| 常用名 | 5-[2,4-二羟基-5-(1-甲基乙基)苯基]-n-乙基-4-[4-(4-吗啉甲基)苯基]-3-异噁唑羧酰胺 | 英文名 | NVP-AUY922 |
|---|---|---|---|
| CAS号 | 747412-49-3 | 分子量 | 465.541 |
| 密度 | 1.2±0.1 g/cm3 | 沸点 | 640.1±55.0 °C at 760 mmHg |
| 分子式 | C26H31N3O5 | 熔点 | N/A |
| MSDS | N/A | 闪点 | 340.9±31.5 °C |
NVP-AUY922 是一种有效的 HSP90 抑制剂，作用于 HSP90α/β，IC50 值分别为 7.8 nM/21 nM，对 GRP94 和 TRAP-1 的作用较弱。
Fields of Application :
AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2.
| CAS Number: | 747412-49-3 |
| Purity: | 99.13% |
| Molecular Weight: | 465.54 |
| Molecular Formula: | C26H31N3O5 |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | AUY 922,AUY-922, NVP-AUY922，NVP-AUY922-NX，AUY922,VER-52296 |
| Chemical Name: | 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide |
| Storage: | 2 years -20°C powder,2 weeks 4°C in DMSO,6 months -80°C in DMSO |
Note: Products for research use only, not for human use
Description:
In vitro:NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value For the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to HSP90. NVP-AUY922 causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex. After the treatment with NVP-AUY922, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFRɑ is decreased. A decrease is also noticed in the expression of Akt and phospho-Akt. Meanwhile, treatment with NVP-AUY922 causes decreased expression of HER-2 in NCI-N87 cells. NVP-AUY922 treatment results in binding of HSP90 to client proteins and setting them up as targets For degradation by the proteasome. NVP-AUY922 can influence cell growth by affecting multiple signaling pathways. In addition, treatment with the proteasome inhibitor, MG132, restores expression of thymidylate synthase, which is decreased by NVP-AUY922. NVP-AUY922 increases the expression of cleaved caspase-3 leading to apoptosis in HSC-2 cells. In vivo:Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model.In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2.For the detailed information of AUY922 (NVP-AUY922), the solubility of AUY922 (NVP-AUY922) in water, the solubility of AUY922 (NVP-AUY922) in DMSO, the solubility of AUY922 (NVP-AUY922) in PBS buffer, the animal experiment (test) of AUY922 (NVP-AUY922), the cell expriment (test) of AUY922 (NVP-AUY922), the in vivo, in vitro and clinical trial test of AUY922 (NVP-AUY922), the EC50, IC50,and Affinity of AUY922 (NVP-AUY922), Please contact DC Chemicals.
