1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. EGFR-IN-12

EGFR-IN-12 是一种 4,6-二取代的嘧啶,是一种有效的,ATP 竞争性,不可逆且高度选择性的 EGFR 抑制剂,IC50 为 21 nM。EGFR-IN-12 还抑制突变型 EGFRL858REGFRL861QIC50 分别为 63 nM 和 4 nM。EGFR-IN-12 对 EGFR 的选择性高于 HER4 (IC50 = 7640 nM) 和 55种其他激酶。EGFR-IN-12 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

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EGFR-IN-12 Chemical Structure

EGFR-IN-12 Chemical Structure

CAS No. : 879127-07-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1980
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1 mg ¥754
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5 mg ¥1800
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10 mg ¥3000
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity[1][2].

IC50 & Target[1]

EGFR (WT)

21 nM (IC50)

EGFRL858R

63 nM (IC50)

EGFRL861Q

4 nM (IC50)

HER4

7640 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-12 (EGFR inhibitor 324674; 0-2 µM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations[2].
EGFR-IN-12 (EGFR inhibitor 324674; 0-3 µM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner[2].
EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 µM and 1.04 µM, respectively[2].
Pretreatment of cells with EGFR-IN-12 (compound 1; 10 µM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HT29 and SW480 cells
Concentration: 0 µM, 1 µM, 2 µM
Incubation Time: 48 hours
Result: Induced apoptosis in HT29 cells and SW480 cells.

Western Blot Analysis[1]

Cell Line: HT29 and SW480 cells
Concentration: 0 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM
Incubation Time: 3 hours
Result: Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.
分子量

413.40

Formula

C21H18F3N5O

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (604.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4190 mL 12.0948 mL 24.1896 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4190 mL 12.0948 mL 24.1896 mL 60.4741 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL 12.0948 mL
10 mM 0.2419 mL 1.2095 mL 2.4190 mL 6.0474 mL
15 mM 0.1613 mL 0.8063 mL 1.6126 mL 4.0316 mL
20 mM 0.1209 mL 0.6047 mL 1.2095 mL 3.0237 mL
25 mM 0.0968 mL 0.4838 mL 0.9676 mL 2.4190 mL
30 mM 0.0806 mL 0.4032 mL 0.8063 mL 2.0158 mL
40 mM 0.0605 mL 0.3024 mL 0.6047 mL 1.5119 mL
50 mM 0.0484 mL 0.2419 mL 0.4838 mL 1.2095 mL
60 mM 0.0403 mL 0.2016 mL 0.4032 mL 1.0079 mL
80 mM 0.0302 mL 0.1512 mL 0.3024 mL 0.7559 mL
100 mM 0.0242 mL 0.1209 mL 0.2419 mL 0.6047 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EGFR-IN-12
目录号:
HY-17499
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