2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Autophagy
  3. PROTACs EGFR Autophagy
  4. PROTAC EGFR degrader 4

PROTAC EGFR degrader 4 是一种有效的 PROTAC 靶向突变 EGFR。PROTAC EGFR degrader 4 诱导 EGFRdel19 和 EGFRL858R/T790M 降解，DC50 值分别为 0.51 和 126 nM。PROTAC EGFR degrader 4 显着抑制 HCC827 和 H1975 细胞系的生长，IC50 值分别为 0.83 和 203.1 nM。诱导 EGFR 降解与自噬 (autophagy) 有关。

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PROTAC EGFR degrader 4 Chemical Structure

PROTAC EGFR degrader 4 Chemical Structure

CAS No. : 2882845-50-1

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5 mg ￥5890
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Customer Review

PROTAC EGFR degrader 4 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
245 nM
Compound: P3
Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
HCC827 IC50
0.76 nM
Compound: P3
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
HepG2 IC50
> 5000 nM
Compound: P3
Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
NCI-H1975 IC50
203 nM
Compound: P3
Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 32883633]
体外研究
(In Vitro)

PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFRdel19) and H1975 (EGFRL858R/T790M) with IC50s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively[1].
PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFRdel19 degradation with a DC50 values of 0.51 nM[1].
PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines[1].
PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase[1].

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

PROTAC EGFR degrader 4 相关抗体:
分子量

995.29

Formula

C55H70N12O4S
CAS 号
性状

固体

颜色

White to off-white

运输条件

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

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (100.47 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 1.0047 mL 5.0237 mL 10.0473 mL
5 mM 0.2009 mL 1.0047 mL 2.0095 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 (protect from light, stored under nitrogen)。-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

PROTAC EGFR degrader 4 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 (protect from light, stored under nitrogen)。-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 1.0047 mL 5.0237 mL 10.0473 mL 25.1183 mL
5 mM 0.2009 mL 1.0047 mL 2.0095 mL 5.0237 mL
10 mM 0.1005 mL 0.5024 mL 1.0047 mL 2.5118 mL
15 mM 0.0670 mL 0.3349 mL 0.6698 mL 1.6746 mL
20 mM 0.0502 mL 0.2512 mL 0.5024 mL 1.2559 mL
25 mM 0.0402 mL 0.2009 mL 0.4019 mL 1.0047 mL
30 mM 0.0335 mL 0.1675 mL 0.3349 mL 0.8373 mL
40 mM 0.0251 mL 0.1256 mL 0.2512 mL 0.6280 mL
50 mM 0.0201 mL 0.1005 mL 0.2009 mL 0.5024 mL
60 mM 0.0167 mL 0.0837 mL 0.1675 mL 0.4186 mL
80 mM 0.0126 mL 0.0628 mL 0.1256 mL 0.3140 mL
100 mM 0.0100 mL 0.0502 mL 0.1005 mL 0.2512 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:

PROTAC EGFR degrader 42882845-50-1PROTAC EGFR degrader4PROTAC EGFR degrader-4PROTACsEGFRAutophagyEpidermal growth factor receptorErbB-1HER1PROTACDegradationInhibitorinhibitorinhibit

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