2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-1 TFA

EGFR-IN-1 TFA 是一种口服活性不可逆的突变型选择性 L858R/T790M EGFR 抑制剂。与野生型 EGFR 相比，EGFR-IN-1 TFA 对 Gefitinib 耐药的 EGFR L858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 TFA 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。

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EGFR-IN-1 TFA Chemical Structure

EGFR-IN-1 TFA Chemical Structure

CAS No. : 2753348-63-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5393
In-stock
1 mg ￥1560
In-stock
5 mg ￥3900
In-stock
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100 mg   询价  

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Customer Review

Other Forms of EGFR-IN-1 TFA:

EGFR-IN-1 TFA 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

IC50 & Target[1]

EGFRL858R/T790M

 

体外研究
(In Vitro)

EGFR-IN-1 TFA (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

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

EGFR-IN-1 TFA 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750)
Concentration: 10 μM
Incubation Time: 72 hours
Result: Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively.
体内研究
(In Vivo)

EGFR-IN-1 TFA (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight[1].
EGFR-IN-1 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1].

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

628.60

Formula

C30H31F3N6O6
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (397.71 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 1.5908 mL 7.9542 mL 15.9084 mL
5 mM 0.3182 mL 1.5908 mL 3.1817 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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

只
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

EGFR-IN-1 TFA 相关分类

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5908 mL 7.9542 mL 15.9084 mL 39.7709 mL
5 mM 0.3182 mL 1.5908 mL 3.1817 mL 7.9542 mL
10 mM 0.1591 mL 0.7954 mL 1.5908 mL 3.9771 mL
15 mM 0.1061 mL 0.5303 mL 1.0606 mL 2.6514 mL
20 mM 0.0795 mL 0.3977 mL 0.7954 mL 1.9885 mL
25 mM 0.0636 mL 0.3182 mL 0.6363 mL 1.5908 mL
30 mM 0.0530 mL 0.2651 mL 0.5303 mL 1.3257 mL
40 mM 0.0398 mL 0.1989 mL 0.3977 mL 0.9943 mL
50 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7954 mL
60 mM 0.0265 mL 0.1326 mL 0.2651 mL 0.6628 mL
80 mM 0.0199 mL 0.0994 mL 0.1989 mL 0.4971 mL
100 mM 0.0159 mL 0.0795 mL 0.1591 mL 0.3977 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.

Keywords:

EGFR-IN-12753348-63-7EGFREpidermal growth factor receptorErbB-1HER1oralnonsmallcelllungcancerNSCLCH1975mutantHCC827phosphorylationInhibitorinhibitorinhibit

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