2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. JBJ-09-063 hydrochloride

JBJ-09-063 hydrochloride 

目录号: HY-147183B 纯度: 99.37%
COA 产品使用指南

摩尔计算器

JBJ-09-063 hydrochloride 是一种突变选择性变构 EGFR 抑制剂，对 EGFR L858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的 IC50 分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 hydrochloride 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 hydrochloride 对 EGFR 酪氨酸激酶抑制剂 (TKI) 敏感和耐药模型均有效。JBJ-09-063 hydrochloride 可用于 EGFR 突变型肺癌研究。

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JBJ-09-063 hydrochloride Chemical Structure

JBJ-09-063 hydrochloride Chemical Structure

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5872
In-stock
1 mg ￥2045
In-stock
5 mg ￥4500
In-stock
10 mg ￥8000
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of JBJ-09-063 hydrochloride:

JBJ-09-063 hydrochloride 相关抗体

Top Publications Citing Use of Products

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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

JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer[1].

IC50 & Target[1]

EGFR L858R

0.147 nM (IC50)

EGFR L858R/T790M

0.063 nM (IC50)

EGFR L858R/T790M/C797S

0.083 nM (IC50)

EGFRLT/L747S

0.396 nM (IC50)

体外研究
(In Vitro)

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations[1].
JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905)[2].

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

JBJ-09-063 hydrochloride 相关抗体:
体内研究
(In Vivo)

JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing[2].

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

Animal Model: Mice[2]
Dosage: 3 mg/kg for i.v., 20 mg/kg for p.o.
Administration: i.v. and p.o.; single dosage
Result: Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
Cl (mL/min/kg), i.v. T1/2 (h) Vss (L/kg) F (%) AUC 8h (ng·h/mL)
15.7 2.3 2.5 15 2398
分子量

593.11

Formula

C31H30ClFN4O3S
性状

固体

颜色

Off-white to light 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
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (168.60 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 1.6860 mL 8.4301 mL 16.8603 mL
5 mM 0.3372 mL 1.6860 mL 3.3721 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

纯度: 99.37%

COA (197 KB) HNMR (238 KB) LCMS (97 KB)

产品使用指南 (1538 KB)
参考文献

JBJ-09-063 hydrochloride 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 1.6860 mL 8.4301 mL 16.8603 mL 42.1507 mL
5 mM 0.3372 mL 1.6860 mL 3.3721 mL 8.4301 mL
10 mM 0.1686 mL 0.8430 mL 1.6860 mL 4.2151 mL
15 mM 0.1124 mL 0.5620 mL 1.1240 mL 2.8100 mL
20 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1075 mL
25 mM 0.0674 mL 0.3372 mL 0.6744 mL 1.6860 mL
30 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4050 mL
40 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0538 mL
50 mM 0.0337 mL 0.1686 mL 0.3372 mL 0.8430 mL
60 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
80 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5269 mL
100 mM 0.0169 mL 0.0843 mL 0.1686 mL 0.4215 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:

JBJ-09-063EGFREpidermal growth factor receptorErbB-1HER1EGFR-mutantlung cancerTKI-sensitiveresistantH3255GRH1975Ba/F3AnticancerInhibitorinhibitorinhibit

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目录号：
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