BI-4020

目录号: HY-129550 纯度: 99.28%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

BI-4020 是一种第四代，具有口服活性，非共价的 EGFR 酪氨酸激酶抑制剂。BI-4020 不仅抑制三联突变的 EGFR del19 T790M C797S 突变体 (在 BaF3 细胞系中，IC₅₀=0.2 nM)，也抑制双重突变的 EGFR del19 T790M 和单突变的 EGFR del19 (IC₅₀=1 nM)。BI-4020 同时保留了针对 EGFR wt 的活性 (IC₅₀=190 nM)。BI-4020 显示高激酶组选择性和良好的 DMPK 特性。

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BI-4020 Chemical Structure

CAS No. : 2664214-60-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥9551	In-stock
1 mg	￥3500	In-stock
5 mg	现货	询价
10 mg		询价
50 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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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

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC₅₀=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC₅₀=1 nM). BI-4020 also shows activity against EGFR wt (IC₅₀=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties^[1].

IC₅₀ & Target^[1]

EGFR^{del19 T790M C797S}

0.2 nM (IC₅₀)

EGFR^{del19 T790M}

EGFR^del19

1 nM (IC₅₀)

EGFR^WT

190 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	200 nM Compound: BI-4020	Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	0.2 nM Compound: BI-4020	Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	0.6 nM Compound: BI-4020	Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay	[PMID: 31689114]
BaF3	IC₅₀	1 nM Compound: BI-4020	Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	11.1 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1100 nM Compound: BI-4020	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	13.1 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1412.1 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	190 nM Compound: BI-4020	Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	1967.5 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2.3 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2.8 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2.8 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	3.4 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	6.5 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	76.4 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	8.8 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	803.7 nM Compound: BI-4020	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
PC-9	IC₅₀	1.3 nM Compound: BI-4020	Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]

体外研究
(In Vitro)

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC₅₀ of 0.6 nM^[1].

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

体内研究
(In Vivo)

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice^[1].

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

分子量

542.68

Formula

C₃₀H₃₈N₈O₂

CAS 号

2664214-60-0

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 250 mg/mL (460.68 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)

1M HCl 中的溶解度 : 100 mg/mL (184.27 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈1))

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8427 mL	9.2135 mL	18.4271 mL
5 mM	0.3685 mL	1.8427 mL	3.6854 mL
10 mM	0.1843 mL	0.9214 mL	1.8427 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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

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

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.28%

选择批次：

Data Sheet (625 KB) SDS (251 KB)

COA (198 KB) LCMS (266 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5. [Content Brief]

BI-4020 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

1M HCl / DMSO	1 mM	1.8427 mL	9.2135 mL	18.4271 mL	46.0677 mL
	5 mM	0.3685 mL	1.8427 mL	3.6854 mL	9.2135 mL
	10 mM	0.1843 mL	0.9214 mL	1.8427 mL	4.6068 mL
	15 mM	0.1228 mL	0.6142 mL	1.2285 mL	3.0712 mL
	20 mM	0.0921 mL	0.4607 mL	0.9214 mL	2.3034 mL
	25 mM	0.0737 mL	0.3685 mL	0.7371 mL	1.8427 mL
	30 mM	0.0614 mL	0.3071 mL	0.6142 mL	1.5356 mL
	40 mM	0.0461 mL	0.2303 mL	0.4607 mL	1.1517 mL
	50 mM	0.0369 mL	0.1843 mL	0.3685 mL	0.9214 mL
	60 mM	0.0307 mL	0.1536 mL	0.3071 mL	0.7678 mL
	80 mM	0.0230 mL	0.1152 mL	0.2303 mL	0.5758 mL
	100 mM	0.0184 mL	0.0921 mL	0.1843 mL	0.4607 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:

BI-40202664214-60-0BI4020BI 4020EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

BI-4020

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