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Tyrphostin RG14620

Tyrphostin RG14620用途

RG14620是 EGFR 抑制剂；IC₅₀ 值为3 μM。

Tyrphostin RG14620名称

[ CAS 号 ]:
136831-49-7

[ 中文名 ]:
RG14620

[ 英文名 ]:
RG14620

[英文别名 ]:

MFCD00236445
RG-14620

Tyrphostin RG14620生物活性

[ 描述 ]:

RG14620是 EGFR 抑制剂；IC50 值为3 μM。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

EGFR:3 μM (IC50, Cell Assay)

[体外研究]

RG14620以剂量依赖性方式抑制由50ng/mL EGF刺激的HER14细胞的集落形成(IC50 =3μM)和DNA合成(IC50 =1μM)。 RG14620还以剂量依赖性方式抑制EGF刺激的MH-85细胞的集落形成(IC50 =4μM)和DNA合成(IC50 =1.25μM)。 RG14620的生长抑制作用不可逆转[2]。

[体内研究]

RG14620,剂量为200μg/小鼠/天,抑制裸鼠体内H-85肿瘤的生长。小鼠表现出较少的恶病质和高钙血症,吃更多的食物,并且比未经治疗的MH-85荷瘤动物更活跃[2]。

[细胞实验]

将MH-85细胞和HER14细胞分别铺在完全培养基中，αMEM或DMEM，补充有10％FCS。过夜培养后，将培养基换成补充有0.2％PCS和50ng / mL EGF（MH-85）的αMEM或补充有0.5％PCS和50ng / mL EGF（HER14）的DMEM。在存在或不存在递增浓度的RG-13022或RG-14620的情况下，将细胞在该培养基中培养10天。在培养结束时，将细胞用4％（v / v）甲醛在不含钙镁的磷酸盐缓冲盐水中在室温下固定15分钟并用苏木精染色。在显微镜下计数每个孔中包括超过20个细胞的集落数[2]。

[动物实验]

小鼠：在MH-85肿瘤接种后1天，每天两次腹膜内注射0.1mL 100％DMSO中的RG14620。对照动物给予相同的载体[1]。

[参考文献]

[1]. Sagara Y, et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15.

[2]. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5.

[相关活性小分子]

Tyrphostin RG14620物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
418.2±45.0 °C at 760 mmHg

[ 熔点 ]:
155 °C

[ 分子式 ]:
C₁₄H₈Cl₂N₂

[ 分子量 ]:
275.133

[ 闪点 ]:
206.7±28.7 °C

[ 精确质量 ]:
274.006439

[ PSA ]:
36.68000

[ LogP ]:
4.47

[ 外观性状 ]:
固体;White to Light yellow powder to crystal

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.657

[ 储存条件 ]:
-20°C;避免加热

Tyrphostin RG14620安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

Tyrphostin RG14620文献

Photoinstability of some tyrphostin drugs: chemical consequences of crystallinity.

Pharm. Res. 12(11) , 1708-15, (1995)

The purpose of this work was to study the photostability of the antiproliferative tyrphostin drug compounds RG 13022(I) and RG 14620(II) as a part of preformulation program.The compounds were exposed ...

Upregulation of retinoic acid receptor-beta by the epidermal growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB pathways.

J. Cell Physiol. 211(3) , 803-15, (2007)

Inhibiting epidermal growth factor-receptor (ErbB-1) represents a powerful anticancer strategy. Activation of retinoid pathways is also in development for cancer treatment. Retinoic acid receptor-beta...

[Effect of signal transduction inhibitors on human endometrial carcinoma cells with differential PTEN gene expression].

Zhonghua Fu Chan Ke Za Zhi 44(9) , 681-5, (2009)

To investigate the apoptotic and proliferation effects of signal transduction inhibitors on human endometrial carcinoma cells with different PTEN gene expression.PTEN antisense oligonucleotide and pcD...

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