首页 工具
登录
购物车
SNX2112

SNX2112

产品编号 T6305   CAS 908112-43-6
别名: SNX-2112, PF 04928473, SNX 2112

SNX2112 (PF 04928473) 是一种具有口服活性的 Hsp90 抑制剂,Kd 为 16 nM。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
SNX2112 Chemical Structure
SNX2112, CAS 908112-43-6
规格 价格/CNY 货期 数量
1 mg ¥ 668 现货
2 mg ¥ 981 现货
5 mg ¥ 1,630 现货
10 mg ¥ 2,250 现货
25 mg ¥ 3,790 现货
50 mg ¥ 5,460 现货
100 mg ¥ 7,670 现货
500 mg ¥ 15,300 现货
1 mL * 10 mM (in DMSO) ¥ 1,810 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: SNX2112 (T6305)
点击图片重新获取验证码
选择批次  
纯度: 99.95%
纯度: 99.46%
纯度: 98.93%
纯度: 98.9%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.
靶点活性 HSP90 β:30 nM(Ka), HSP90 α:30 nM(Ka)
体外活性 Treatment of BT-474 cells with 1 μM SNX-2112 results in down-regulation of HER2 expression within 3 to 6 hours of drug exposure with near-complete loss of HER2 expression by 10 hours. Treatment with SNX-2112 also results in a decline in total Akt expression. SNX-2112 inhibits cell proliferation with IC50 values ranging from 10 to 50 nM, in BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells. And these antiproliferative effects are associated with hypophosphorylation of Rb, arrest of G1 and modest levels of apotosis. [1] SNX-2112 competitively binds to the N-terminal adenosine triphosphate binding site of Hsp90. SNX-2112 induces apoptosis via caspase-8, -9, -3, and poly (ADPribose) polymerase cleavage. SNX-2112 inhibits cytokine-inducedAkt and extracellular signal-related kinase (ERK) activation and also overcomes the growth advantages conferred by interleukin-6, insulin-like growth factor-1, and bone marrow stromal cells. SNX-2112 inhibits tube formation by human umbilical vein endothelial cells via abrogation of eNOS/Akt pathway and markedly inhibits osteoclast formation via down-regulation of ERK/c-fos and PU.1. [2] Cell lines (eight cell lines from osteosarcoma, neuroblastoma, hepatoblastoma, and ymphoma) studied demonstrates sensitivity to SNX-2112 with IC50 values ranging from 10-100?nM. A higher dose (70?nM) exhibits a more prolonged inhibition and larger sub-G1 accumulation. Observed levels of Akt1 and C-Raf are markedly reduced over time along with an increase in PARP cleavage. [3] A recent research indicates NX-2112 induces autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and utophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent. [4]
体内活性 SNX-2112, delivered by its prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model and blockade of Hsp90 by SNX-2112 not only inhibits MM cell growth but also acts in the bone marrow microenvironment to block angiogenesis and osteoclastogenesis. [2]
激酶实验 ATP Displacement Assay: For the protein affinity-displacement assay, a purine-based affinity resin is generated by incubating ATP-linked Sepharose with Jurkat cell lysate (flash frozen and homogenized in saline) at 4 °C. This is then incubated with SNX-2112 for 90 minutes. Proteins eluted by drug are then resolved by SDS-PAGE, visualized with silver staining, and excised from the gel for MS-based identification. Briefly, after destaining and trypsin digestion, peptides are extracted with μC18 ZipTips and then eluted and spotted directly to a conventional stainless steel matrix-assisted laser desorption/ionization target with a saturated solution of α-cyano-4- hydroxycinnamic acid in 50% acetonitrile, 0.15% formic acid. Mass spectra are then acquired using a MALDI-TOF/TOF 4700 Proteomics Analyzer. MS spectra are acquired (1,000 shots per spectrum), and the three peaks from each with the greatest signal-to-noise ratio are automatically submitted for tandem MS analysis (3000 shots per spectrum). The collision energy is 1keV. Air is used as the collision gas. Protein identification is done from the MS and tandem MS data using GPS Explorer software with the integrated Mascot database search engine.
细胞实验 Cell viability is determined by seeding 2-5 × 103 cells per well in 96- well plates and treating with SNX-2112 24 hours after plating in complete medium (200 μL). Each drug concentration is tested in eight wells. Cells are assayed using the Alamar blue viability test after a 96-h incubation. Flow cytometry is done using nuclei stained with ethidium bromide and isolated via the Nusse protocol(Only for Reference)
别名 SNX-2112, PF 04928473, SNX 2112
分子量 464.48
分子式 C23H27F3N4O3
CAS No. 908112-43-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 1 mg/mL (2.15 mM)

DMSO: 86 mg/mL (185.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1529 mL 10.7647 mL 21.5295 mL 53.8236 mL
DMSO 5 mM 0.4306 mL 2.1529 mL 4.3059 mL 10.7647 mL
10 mM 0.2153 mL 1.0765 mL 2.1529 mL 5.3824 mL
20 mM 0.1076 mL 0.5382 mL 1.0765 mL 2.6912 mL
50 mM 0.0431 mL 0.2153 mL 0.4306 mL 1.0765 mL
100 mM 0.0215 mL 0.1076 mL 0.2153 mL 0.5382 mL

TargetMol Calculator计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

TargetMol Library Books参考文献

1. Chandarlapaty S, et al, Clin Cancer Res, 2008, 14(1), 240-248. 2. Okawa Y, et al, Blood, 2009, 113(4), 846-855. 3. Chinn DC, et al, Pediatr Blood Cancer, 2012, 58(6), 885-890. 4. Liu KS, et al, Cancer Lett, 2012, 318(2), 180-188.

TargetMol Library Books文献引用

1. Zhao D, Xu Y M, Cao L Q, et al. Complex Crystal Structure Determination and in vitro Anti–non–small Cell Lung Cancer Activity of Hsp90N Inhibitor SNX-2112. Frontiers in cell and developmental biology. 2021, 9: 567. 2. Zhao D, Xu Y M, Cao L Q, et al. Complex Crystal Structure Determination and in vitro Anti–non–small Cell Lung Cancer Activity of Hsp90N Inhibitor SNX-2112. Frontiers in cell and developmental biology. 2021, 9: 567.
CC-99677 HSP90-IN-22 Eupalinolide A PU-H71 HCl Grp94 Inhibitor-1 Myricanone KU-32 HSP27 inhibitor J2

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抑制剂库 临床前化合物库 血液病分子库 HIF-1化合物库 内质网应激化合物库 细胞凋亡化合物库 细胞骨架化合物库 代谢化合物库 抗代谢疾病化合物库

TargetMol Calculator剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

TargetMol Calculator 体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SNX2112 908112-43-6 Cytoskeletal Signaling Metabolism HSP PF04928473 SNX-2112 PF-04928473 PF 04928473 SNX 2112 Inhibitor inhibitor inhibit

 

TargetMol Loading
陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼