多肽定制EGFR-derived peptide 编码

上海金畔生物科技有限公司可以定制不同序列多肽,可以访问官网了解更多产品信息。

名称 EGFR-derived peptide
编码
别名 EGFR-derived peptide
纯度 80%,90%,95%,98%,99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列(单字母缩写) LVEPLTPSGEAPNQK
序列(三字母缩写) Leu-Val-Glu-Pro-Leu-Thr-Pro-Ser-Gly-Glu-Ala-Pro-Asn-Gln-Lys
基本描述
溶解度
分子量 1579.78
化学式 C69H114N18O24
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents EGFR-derived peptide          编码
Figures EGFR-derived peptide          编码
Reference
C端
N端
化学桥

Sunvozertinib(Synonyms: DZD9008)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Sunvozertinib (Synonyms: DZD9008) 纯度: 99.71%

Sunvozertinib (DZD9008) 是一种有效的 ErbBs (EGFR、Her2,尤其是突变型) 和 BTK 抑制剂。Sunvozertinib 显示 EGFR 外显子 20 NPH 插入、EGFR 外显子 20 ASV 插入、EGFR L858R 和 T790M 突变以及 Her2 外显子 20 YVMA 和 EGFR WT A431 的 IC50 分别为 20.4、20.4、1.1、7.5 和 80.4 nM (详细信息请参考专利 WO2019149164A1, example 52)。

Sunvozertinib(Synonyms: DZD9008)

Sunvozertinib Chemical Structure

CAS No. : 2370013-12-8

规格 价格 是否有货 数量
5 mg ¥4800 In-stock
10 mg ¥8000 In-stock
25 mg ¥16500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Sunvozertinib 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52)[1].

IC50 & Target[1]

EGFR exon 20 insertion

20.4 nM (IC50)

EGFRL858R/T790M

1.1 nM (IC50)

Her2 Exon20 YVMA

7.5 nM (IC50)

体外研究
(In Vitro)

Sunvozertinib shows GI50s of 60.4, 83.2, 3.3, 101.3, and 47.1 nM for EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively. Sunvozertinib shows GI50s of 3.2, 5.8, 51.3, and 1983.5 nM for BTK WT OCI-LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, respectively[1].
Sunvozertinib inhibits p-BTK with IC50 of 1.6 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

584.08

Formula

C29H35ClFN7O3

CAS 号

2370013-12-8

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
In Vitro: 

DMSO : 100 mg/mL (171.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7121 mL 8.5605 mL 17.1209 mL
5 mM 0.3424 mL 1.7121 mL 3.4242 mL
10 mM 0.1712 mL 0.8560 mL 1.7121 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.28 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.28 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.28 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR-IN-12

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR-IN-12  纯度: 99.49%

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。

EGFR-IN-12

EGFR-IN-12 Chemical Structure

CAS No. : 879127-07-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1980 In-stock
5 mg ¥1800 In-stock
10 mg ¥3000 In-stock
25 mg ¥6000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-12 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

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

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].

上海金畔生物科技有限公司 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

879127-07-8

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (604.74 mM; Need ultrasonic)

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
10 mM 0.2419 mL 1.2095 mL 2.4190 mL

*

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。

参考文献
  • [1]. Qiong Zhang, et al. Discovery of EGFR Selective 4,6-disubstituted Pyrimidines From a Combinatorial Kinase-Directed Heterocycle Library. J Am Chem Soc. 2006 Feb 22;128(7):2182-3.

    [2]. Zhiwei Yu, et al. Novel Irreversible EGFR Tyrosine Kinase Inhibitor 324674 Sensitizes Human Colon Carcinoma HT29 and SW480 Cells to Apoptosis by Blocking the EGFR Pathway. Biochem Biophys Res Commun. 2011 Aug 12;411(4):751-6.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Mutated EGFR-IN-1(Synonyms: Osimertinib analog)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Mutated EGFR-IN-1 (Synonyms: Osimertinib analog) 纯度: 99.36%

Mutated EGFR-IN-1 (Osimertinib analog) 是突变型 EGFR (L858R EGFR,Exonl9缺失活化突变和T790M抗性突变) 抑制剂的中间体。

Mutated EGFR-IN-1(Synonyms: Osimertinib analog)

Mutated EGFR-IN-1 Chemical Structure

CAS No. : 1421372-66-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1470 In-stock
2 mg ¥1000 In-stock
5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
50 mg ¥5500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Mutated EGFR-IN-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant. IC50 value: Target: Mutated EGFR inhibitor More information can be found in Patent WO 2013014448 A1.2 – (2, 4, 5 – substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer.

IC50 & Target[1]

EGFRL858R

 

EGFRExon 19 deletion/T790M

 

EGFRT790M

 

分子量

445.56

Formula

C25H31N7O

CAS 号

1421372-66-8

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 75 mg/mL (168.33 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2444 mL 11.2218 mL 22.4437 mL
5 mM 0.4489 mL 2.2444 mL 4.4887 mL
10 mM 0.2244 mL 1.1222 mL 2.2444 mL

*

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。

参考文献
  • [1]. Patent WO 2013014448 A1. 2 – (2, 4, 5 – substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer .

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Theliatinib(Synonyms: 西利替尼; Xiliertinib; HMPL-309)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Theliatinib (Synonyms: 西利替尼; Xiliertinib; HMPL-309) 纯度: 99.88%

Theliatinib (Xiliertinib) 是一种有效、ATP 竞争性、口服活性和高度选择性的 EGFR 抑制剂,Ki 为 0.05 nM,IC50 为 3 nM。Theliatinib 对 EGFR T790M/L858R 突变体的 IC50 值为 22 nM。Theliatinib 对 EGFR 的选择性是其他激酶的 50 倍以上。抗肿瘤活性。

Theliatinib(Synonyms: 西利替尼; Xiliertinib;  HMPL-309)

Theliatinib Chemical Structure

CAS No. : 1353644-70-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1947 In-stock
1 mg ¥680 In-stock
5 mg ¥2000 In-stock
10 mg ¥3250 In-stock
25 mg ¥6500 In-stock
50 mg ¥11000 In-stock
100 mg ¥19000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Theliatinib 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity[1].

IC50 & Target[1]

EGFR

3 nM (IC50)

EGFR

0.05 nM (Ki)

EGFR (L858R/T790M)

22 nM (IC50)

体外研究
(In Vitro)

Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC50 of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC50 values of 80 nM, 58 nM and 354 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)[1]
Dosage: 2 mg/kg, 5 mg/kg, 15 mg/kg
Administration: Oral administration;daily; for 21 days
Result: Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.

Clinical Trial

分子量

442.51

Formula

C25H26N6O2

CAS 号

1353644-70-8

中文名称

西利替尼

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (11.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2598 mL 11.2992 mL 22.5984 mL
5 mM 0.4520 mL 2.2598 mL 4.5197 mL
10 mM 0.2260 mL 1.1299 mL 2.2598 mL

*

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。

参考文献
  • [1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR/ErbB-2/ErbB-4 inhibitor-2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR/ErbB-2/ErbB-4 inhibitor-2  纯度: 99.69%

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) 是一种 EGFRErbB 抑制剂,IC50 分别为 0.017 μM,0.08 μM,1.91 μM。

EGFR/ErbB-2/ErbB-4 inhibitor-2

EGFR/ErbB-2/ErbB-4 inhibitor-2 Chemical Structure

CAS No. : 179248-61-4

规格 价格 是否有货 数量
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

EGFR/ErbB-2/ErbB-4 inhibitor-2 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM[1].

IC50 & Target[1]

EGFR

0.017 μM (IC50)

ErbB2

0.08 μM (IC50)

ErbB4

1.91 μM (IC50)

体外研究
(In Vitro)

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) also inhibits c-Src, VEGFR2, c-Fms and with IC50s of 0.30, 2.2, and 14.0 μM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

387.43

Formula

C23H21N3O3

CAS 号

179248-61-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (86.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL

*

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)。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.45 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Perry S Brignola, et al. Comparison of the biochemical and kinetic properties of the type 1 receptor tyrosine kinase intracellular domains. Demonstration of differential sensitivity to kinase inhibitors. J Biol Chem. 2002 Jan 11;277(2):1576-85.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR-IN-1 TFA

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR-IN-1 TFA  纯度: 99.05%

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。

EGFR-IN-1 TFA

EGFR-IN-1 TFA Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6640 In-stock
5 mg ¥4800 In-stock
10 mg ¥8000 In-stock
25 mg ¥17000 In-stock
50 mg ¥28000 In-stock
100 mg ¥43000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-1 TFA 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Orally Active Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

628.60

Formula

C30H31F3N6O6

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
In Vitro: 

DMSO : 250 mg/mL (397.71 mM; Need ultrasonic)

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
10 mM 0.1591 mL 0.7954 mL 1.5908 mL

*

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。

参考文献
  • [1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Naquotinib(Synonyms: ASP8273)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Naquotinib (Synonyms: ASP8273)

Naquotinib (ASP8273) 是有口服活性,不可逆的 EGFR 突变体抑制剂;对EGFR突变体和EGFR的 IC50 值分别为8-33和230 nM。

Naquotinib(Synonyms: ASP8273)

Naquotinib Chemical Structure

CAS No. : 1448232-80-1

规格 价格 是否有货
50 mg ¥7800 询问价格 & 货期

* Please select Quantity before adding items.

Naquotinib 的其他形式现货产品:

Naquotinib mesylate

生物活性

Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

IC50 & Target[1]

EGFR

230 nM (IC50)

EGFRT790M

 

EGFRL858R/T790M

 

EGFRL858R

 

EGFRExon 19 deletion/T790M

 

体外研究
(In Vitro)

In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s of 8-33 nM[1]. Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

562.71

Formula

C30H42N8O3

CAS 号

1448232-80-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1728. doi:10.1158/1538-7445.AM2014-1728

    [2]. Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2586. doi:10.1158/1538-7445.AM2015-2586

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

WZ8040

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

WZ8040  纯度: 99.22%

WZ8040 是不可逆的、突变的 EGFR T790M 的抑制剂,可以抑制 EGFR 磷酸化。WZ8040 对突变型EGFR的活性是野生型EGFR 的100倍以上。

WZ8040

WZ8040 Chemical Structure

CAS No. : 1214265-57-2

规格 价格 是否有货 数量
5 mg ¥3900 In-stock
10 mg ¥6500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

WZ8040 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal[1].

IC50 & Target

EGFR Del E746_A750

1 nM (IC50, in HCC827 cells)

EGFR Del E746_A750

6 nM (IC50, in PC9 cells)

EGFR L858R

66 nM (IC50, in H3255 cells )

EGFR L858R/T790M

9 nM (IC50, in H1975 cells)

EGFR Del E746_A750/T790M

8 nM (IC50, in PC9 GR cells)

EGFR E746_A750/MET amp

>3.3 μM (IC50, in HCC827 GR cells)

ERBB2 amp

738 nM (IC50, in H1819 cells)

ERBB2 amp

915 nM (IC50, in Calu-3 cells)

ERBB2 Ins G776V, C

744 nM (IC50, in H1781 cells)

EGFR & ERBB2 WT

1.82 μM (IC50, in HN11 cells)

体外研究
(In Vitro)

WZ8040 exhibits IC50 values of 1 nM for HCC827 (EGFR Del E746_A750), 6 nM for PC9 (EGFR Del E746_A750), 66 nM for H3255 (EGFR L858R), 9 nM for H1975 (EGFR L858R/T790M), 8 nM for PC9 GR (EGFR Del E746_A750/T790M), >3.3 μM for HCC827 GR (EGFR E746_A750/MET amp), 738 nM for H1819 (ERBB2 amp), 915 nM for Calu-3 (ERBB2 amp), 744 nM for H1781 (ERBB2 Ins G776V, C), 1.82 μM for HN11 (EGFR & ERBB2 WT), respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NSCLC cell lines and Ba/F3 cells.
Concentration: 0-3.3 μM.
Incubation Time: 24 hours.
Result: Exhibited activity for EGFR-mutated NSCLC lines, such as HH827, PC9, H3255, H1819, Calu-3, H1781 and HN11 cells.

分子量

481.01

Formula

C24H25ClN6OS

CAS 号

1214265-57-2

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (51.97 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0790 mL 10.3948 mL 20.7896 mL
5 mM 0.4158 mL 2.0790 mL 4.1579 mL
10 mM 0.2079 mL 1.0395 mL 2.0790 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.08 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.08 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

BAY 2476568

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BAY 2476568 

BAY 2476568 是一种高效、选择性的 EGFR 抑制剂,对野生型 EGFR 和突变型 EGFR 作用的 IC50 值为 < 0.2 nM。

BAY 2476568

BAY 2476568 Chemical Structure

CAS No. : 2311901-93-4

规格 价格 是否有货
5 mg ¥7500 询问价格 & 货期
10 mg ¥12000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG)[1].

分子量

454.49

Formula

C24H27FN4O4

CAS 号

2311901-93-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Stephan Siegel, et al. 4h-pyrrolo[3,2-c]pyridin-4-one derivatives. WO2019081486A1.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

BLU-945

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BLU-945 

BLU-945 是一种有效的选择性表皮生长因子受体 (EGFR) 抑制剂。EGFR是erbB受体家族的成员,该家族包括跨膜蛋白酪氨酸激酶受体。BLU-945 有效抑制具有 L858R 和/或外显子 19 缺失突变、T790M 突变和 C797S 突变的 EGFR。BLU-945 有助于有效给药并降低 EGFR 介导的靶向毒性。BLU-945 具有研究癌症疾病的潜力 (信息提取自专利 WO2021133809A1,化合物 112)。

BLU-945

BLU-945 Chemical Structure

CAS No. : 2660250-10-0

规格 价格 是否有货
5 mg ¥15200 询问价格 & 货期
10 mg ¥24800 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

receptor (EGFR). EGFR is a member of the erbB receptor family, which includes transmembrane protein tyrosine kinase receptors. BLU-945 effectively inhibits EGFR with L858R and/or exon 19 deletion mutation, T790M mutation, and C797S mutation. BLU-945 facilitates efficacious dosing and reduces EGFR-mediated on-target toxicities. S BLU-945 has the potential for the research of cancer disease (extracted from patent WO2021133809A1, compound 112)[1].

分子量

556.70

Formula

C28H37FN6O3S

CAS 号

2660250-10-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

MS9427

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MS9427 

MS9427 是一种有效的 PROTAC EGFR 降解剂,对野生型 EGFR 和突变型 EGFR L858R 的 Kd 分别为 7.1 nM 和 4.3 nM。MS9427 通过泛素/蛋白酶体系统 (UPS) 和自噬/溶酶体途径有效诱导突变型 EGFRs 降解。MS9427 对 NSCLC 细胞增殖有较强的抑制作用。MS9427 可用于抗癌研究。

MS9427

MS9427 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer[1].

IC50 & Target[1]

EGFR (WT)

7.1 nM (Kd)

EGFR L858R

4.3 nM (Kd)

体外研究
(In Vitro)

MS9427 has antiproliferative activity against HCC-827 cells with a GI50 of 0.87 ± 0.27 μM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

993.47

Formula

C48H58ClFN8O12

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yu X, et al. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J Med Chem. 2022 Jun 23;65(12):8416-8443.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR Protein Tyrosine Kinase Substrate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR Protein Tyrosine Kinase Substrate 

EGFR Protein Tyrosine Kinase Substrate 是EGFR 酪氨酸激酶的底物。

EGFR Protein Tyrosine Kinase Substrate

EGFR Protein Tyrosine Kinase Substrate Chemical Structure

CAS No. : 945830-38-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.

分子量

1076.16

Formula

C48H73N11O17

CAS 号

945830-38-6

Sequence

Ala-Asp-Glu-Tyr-Leu-Ile-Pro-Gln-Gln

Sequence Shortening

ADEYLIPQQ

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR Protein Tyrosine Kinase Substrate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR Protein Tyrosine Kinase Substrate 

EGFR Protein Tyrosine Kinase Substrate 是EGFR 酪氨酸激酶的底物。

EGFR Protein Tyrosine Kinase Substrate

EGFR Protein Tyrosine Kinase Substrate Chemical Structure

CAS No. : 945830-38-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.

分子量

1076.16

Formula

C48H73N11O17

CAS 号

945830-38-6

Sequence

Ala-Asp-Glu-Tyr-Leu-Ile-Pro-Gln-Gln

Sequence Shortening

ADEYLIPQQ

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EGFR Protein Tyrosine Kinase Substrate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EGFR Protein Tyrosine Kinase Substrate 

EGFR Protein Tyrosine Kinase Substrate 是EGFR 酪氨酸激酶的底物。

EGFR Protein Tyrosine Kinase Substrate

EGFR Protein Tyrosine Kinase Substrate Chemical Structure

CAS No. : 945830-38-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.

分子量

1076.16

Formula

C48H73N11O17

CAS 号

945830-38-6

Sequence

Ala-Asp-Glu-Tyr-Leu-Ile-Pro-Gln-Gln

Sequence Shortening

ADEYLIPQQ

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EMI1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EMI1 

EMI1 是 EGFR 三重突变体 EGFR ex19del/T790M/C797SEGFR L858R/T790M/C797S 的有效抑制剂。EMI1 可用于与 EGFR 突变相关的耐药型非小细胞肺癌 (NSCLC) 的研究。

EMI1

EMI1 Chemical Structure

CAS No. : 35773-42-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

 

EGFRL858R/T790M/C797S

 

体外研究
(In Vitro)

EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM[1].
EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1[1].
EMI1 (1 nM-100μM) strongly inhibits the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PC9 EGFR ex19del/T790M/C797S and HBE bronchial epithelial lung EGFR-WT control cells.
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Strongly inhibited the viability.

分子量

334.37

Formula

C20H18N2O3

CAS 号

35773-42-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Punit Saraon, et al. A drug discovery platform to identify compounds that inhibit EGFR triple mutants. Nat Chem Biol. 2020 May;16(5):577-586.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EMI1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EMI1 

EMI1 是 EGFR 三重突变体 EGFR ex19del/T790M/C797SEGFR L858R/T790M/C797S 的有效抑制剂。EMI1 可用于与 EGFR 突变相关的耐药型非小细胞肺癌 (NSCLC) 的研究。

EMI1

EMI1 Chemical Structure

CAS No. : 35773-42-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

 

EGFRL858R/T790M/C797S

 

体外研究
(In Vitro)

EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM[1].
EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1[1].
EMI1 (1 nM-100μM) strongly inhibits the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PC9 EGFR ex19del/T790M/C797S and HBE bronchial epithelial lung EGFR-WT control cells.
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Strongly inhibited the viability.

分子量

334.37

Formula

C20H18N2O3

CAS 号

35773-42-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Punit Saraon, et al. A drug discovery platform to identify compounds that inhibit EGFR triple mutants. Nat Chem Biol. 2020 May;16(5):577-586.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

EMI1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EMI1 

EMI1 是 EGFR 三重突变体 EGFR ex19del/T790M/C797SEGFR L858R/T790M/C797S 的有效抑制剂。EMI1 可用于与 EGFR 突变相关的耐药型非小细胞肺癌 (NSCLC) 的研究。

EMI1

EMI1 Chemical Structure

CAS No. : 35773-42-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

 

EGFRL858R/T790M/C797S

 

体外研究
(In Vitro)

EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM[1].
EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1[1].
EMI1 (1 nM-100μM) strongly inhibits the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PC9 EGFR ex19del/T790M/C797S and HBE bronchial epithelial lung EGFR-WT control cells.
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Strongly inhibited the viability.

分子量

334.37

Formula

C20H18N2O3

CAS 号

35773-42-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Punit Saraon, et al. A drug discovery platform to identify compounds that inhibit EGFR triple mutants. Nat Chem Biol. 2020 May;16(5):577-586.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

PF-6274484

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PF-6274484  纯度: 98.41%

PF-6274484 是一种有效的 EGFR 抑制剂,对于 EGFR-L858R/T790M 和 WT-EGFR,Kis 分别为 0.14 nM 和 0.18 nM。PF-6274484 在 H1975 肿瘤细胞和 A549 肿瘤细胞中抑制EGFR-L858R/T790M自身磷酸化和EGFR-WT,IC50 分别为6.6和5.8 nM。

PF-6274484

PF-6274484 Chemical Structure

CAS No. : 1035638-91-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1150 In-stock
25 mg ¥2400 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PF-6274484 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively[1].

IC50 & Target[1]

EGFR (WT)

0.18 nM (Ki)

EGFRL858R/T790M

0.14 nM (Ki)

分子量

372.78

Formula

C18H14ClFN4O2

CAS 号

1035638-91-5

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (67.06 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6825 mL 13.4127 mL 26.8255 mL
5 mM 0.5365 mL 2.6825 mL 5.3651 mL
10 mM 0.2683 mL 1.3413 mL 2.6825 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.58 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Schwartz PA, et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc Natl Acad Sci U S A. 2014;111(1):173-178.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

PF-6274484

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PF-6274484  纯度: 98.41%

PF-6274484 是一种有效的 EGFR 抑制剂,对于 EGFR-L858R/T790M 和 WT-EGFR,Kis 分别为 0.14 nM 和 0.18 nM。PF-6274484 在 H1975 肿瘤细胞和 A549 肿瘤细胞中抑制EGFR-L858R/T790M自身磷酸化和EGFR-WT,IC50 分别为6.6和5.8 nM。

PF-6274484

PF-6274484 Chemical Structure

CAS No. : 1035638-91-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1150 In-stock
25 mg ¥2400 In-stock
50 mg ¥4500 In-stock
100 mg ¥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PF-6274484 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively[1].

IC50 & Target[1]

EGFR (WT)

0.18 nM (Ki)

EGFRL858R/T790M

0.14 nM (Ki)

分子量

372.78

Formula

C18H14ClFN4O2

CAS 号

1035638-91-5

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (67.06 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6825 mL 13.4127 mL 26.8255 mL
5 mM 0.5365 mL 2.6825 mL 5.3651 mL
10 mM 0.2683 mL 1.3413 mL 2.6825 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.58 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Schwartz PA, et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc Natl Acad Sci U S A. 2014;111(1):173-178.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务