2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. PROTACs EGFR
  4. DDC-01-163

DDC-01-163 是一种选择性作用于 EGFR 突变体的 PROTAC 降解剂，其 IC50 为 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658))。

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DDC-01-163

DDC-01-163 Chemical Structure

CAS No. : 2140806-84-2

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规格 价格 是否有货 数量
1 mg ￥1650
In-stock
5 mg ￥4105
In-stock
10 mg 现货 询价
25 mg 询价 询价
50 mg   询价  
100 mg   询价  

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Customer Review

DDC-01-163 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 EGFR 亚型特异性产品:

查看所有亚型
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

DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC50 of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658))[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 EC50
< 500 nM
Compound: Example I-22
Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay
Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay
[PMID: 31413790]
BaF3 IC50
28 nM
Compound: Fig 1, Cpd 7
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
[PMID: 35691176]
BaF3 IC50
41 nM
Compound: 5
Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation
[PMID: 35254067]
BaF3 IC50
41 nM
Compound: Fig 1, Cpd 7
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
[PMID: 35691176]
BaF3 IC50
50 nM
Compound: Fig 1, Cpd 7
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
[PMID: 35691176]
BaF3 IC50
96 nM
Compound: 14
Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth
Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth
[PMID: 35728507]
BaF3 IC50
96 nM
Compound: 5
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
[PMID: 35254067]
BaF3 IC50
96 nM
Compound: DDC-01-163
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs
[PMID: 36274273]
体外研究
(In Vitro)

DDC-01-163 (0-10 μM) 浓度依赖性地抑制了 L858R/T790M EGFR 突变体 Ba/F3 细胞的增殖，而对野生型 EGFR-Ba/F3 细胞无影响[1]。
DDC-01-163在 L858R/T790M 细胞中对 EGFR 显示出IC50/EC50值为96 nM[2]。

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

DDC-01-163 相关抗体:
分子量

942.05

Formula

C49H51N9O9S
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (53.08 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 1.0615 mL 5.3076 mL 10.6151 mL
5 mM 0.2123 mL 1.0615 mL 2.1230 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。-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

DDC-01-163 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。-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 1.0615 mL 5.3076 mL 10.6151 mL 26.5379 mL
5 mM 0.2123 mL 1.0615 mL 2.1230 mL 5.3076 mL
10 mM 0.1062 mL 0.5308 mL 1.0615 mL 2.6538 mL
15 mM 0.0708 mL 0.3538 mL 0.7077 mL 1.7692 mL
20 mM 0.0531 mL 0.2654 mL 0.5308 mL 1.3269 mL
25 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0615 mL
30 mM 0.0354 mL 0.1769 mL 0.3538 mL 0.8846 mL
40 mM 0.0265 mL 0.1327 mL 0.2654 mL 0.6634 mL
50 mM 0.0212 mL 0.1062 mL 0.2123 mL 0.5308 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:

DDC-01-1632140806-84-2PROTACsEGFREpidermal growth factor receptorErbB-1HER1CRBNBa/F3L858R/T790MInhibitorinhibitorinhibit

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目录号：
HY-139997
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