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Tyrphostin AG 879

Tyrphostin AG 879 (AG 879) 是一种抑制TrKA 磷酸化的酪氨酸激酶抑制剂，IC50为 10 μM。它还是一种选择性ErbB2酪氨酸激酶抑制剂，IC50为 1 μM，具有抗癌活性。

CAS号

148741-30-4

分子式

C18H24N2OS

主要靶点

Apoptosis|EGFR|PDGFR|HER|Trk receptor

仅限科研使用

Cat No : CM04458

Print datasheet

Synonyms

AG 879

验证数据展示

  • CAS No.: 148741-30-4

    Tyrphostin AG 879
    CAS#: 148741-30-4

产品信息

Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.

CAS号 148741-30-4
分子式 C18H24N2OS
主要靶点 Apoptosis|EGFR|PDGFR|HER|Trk receptor
主要通路 JAK/STAT信号通路|凋亡|蛋白酪氨酸激酶|血管生成
分子量 316.46
纯度 99.05%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 AG 879

靶点活性

HER2/ErbB2:1 μM

体内活性

AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. [4] AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells. [5]

体外活性

AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. [1] AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. [2] AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. [3] AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937). [4]

溶解度

DMSO:31.7 mg/mL (100 mM),Ethanol:7.9 mg/mL (25 mM)

细胞实验

Cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.(Only for Reference)

参考文献

1.Zhou Y, et al. Cancer Res, 2005, 65(13), 5848-5856.
2.He H, et al. Cancer Biol Ther, 2004, 3(1), 96-101.
3.Larsson LI, et al. Cell Mol Life Sci, 2004, 61(19-20), 2624-2631.
4.Rende M, et al. Anticancer Drugs, 2006, 17(8), 929-941.
5.He H, et al. Cancer J, 2001, 7(3), 191-202.
6.Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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=
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C1   V1   C2   V2