2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. BGB-102

BGB-102  (Synonyms: JNJ-26483327)

目录号: HY-15732
COA 产品使用指南

摩尔计算器

BGB-102 是多重激酶抑制剂，能够抑制 EGFR，HER2 和 HER4，IC50 值分别为 9.6 nM，18 nM 和 40.3 nM。

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BGB-102 Chemical Structure

BGB-102 Chemical Structure

CAS No. : 807640-87-5

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BGB-102 相关抗体

Top Publications Citing Use of Products

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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.

IC50 & Target[1]

EGFR

9.6 nM (IC50)

HER2

18 nM (IC50)

HER4

40.3 nM (IC50)

体外研究
(In Vitro)

JNJ-26483327 (5 µM or 10 µM) with Herceptin treatment decreases HER2 phosphorylation in SKBR3 cells. JNJ-26483327 exerts greater inhibition of cell viability after 3, 6, or 8 d of treatment compared to Herceptin or JNJ-26483327 alone. JNJ-26483327 with TAPI-1 exerts less cell viability inhibition than Herceptin alone in both SKBR3 and BT474 cells[1].

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

BGB-102 相关抗体:
体内研究
(In Vivo)

JNJ-26483327 (75 mg/kg, p.o.) delays xenograft tumour growth compared to vehicle treatment, but when combines with Herceptin, they can abrogate the PKB feedback loop and is synergistic in inhibition of xenograft tumour growth[1].

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

457.36

Formula

C22H25BrN4O2
CAS 号
Unlabeled CAS

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

THF 中的溶解度 : ≥ 7.27 mg/mL (15.90 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 2.1865 mL 10.9323 mL 21.8646 mL
5 mM 0.4373 mL 2.1865 mL 4.3729 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
Cell Assay
[1]

SKBR3 and BT474 cells are grown in 24-well plates after seeding approximately 20,000 cells per well. The cells are grown for at least 24 h before treatment with 40 µg/mL Herceptin, 5 µM JNJ-26483327, 10 µM TAPI-1, 10 µM ADAM17 inhibitor, or a combination of these drugs for different durations. For the exogenous ligand experiments, 100 ng/mL EGF, heregulin, or betacellulin is added to the cells in addition to Herceptin (40 µg/mL) for a total of 5 d in BT474 cells. On the day of the experiment, the cells are trypsinized and diluted with PBS. The viable cells are counted using a cell counter.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Human BT474 breast tumour cells are injected directly into the inguinal region of the male NMRI Nude mice (1×107 cells/200 mL/animal) on day 0. On day 25, when the tumour volume has reached an approximate average of 200 mm3, mice are randomized according to tumour volume, with ten mice per treatment group. Mice are then treated twice daily with either vehicle (30% Captisol) or vehicle containing JNJ-26483327 (75 mg/kg twice daily) by gavage (p.o.) for 21 d. Alternatively, mice are treated twice weekly with either vehicle (0.9% [w/v] NaCl) or a vehicle containing Herceptin (10 mg/kg) by intraperitoneal injection administered in a volume of 10 mL/kg body weight, for three cycles (i.e., 21 d). Another group receives combined doses of both agents. Tumour size and body weights are measured twice weekly, with mice monitored daily for clinical signs of toxicity for the duration of the treatment. Clinical signs of toxicity included (but are not limited to) persistent anorexia or dehydration, morbidity, lethargy, hypothermia, and/or laboured respiration.

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

BGB-102 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
THF 1 mM 2.1865 mL 10.9323 mL 21.8646 mL 54.6615 mL
5 mM 0.4373 mL 2.1865 mL 4.3729 mL 10.9323 mL
10 mM 0.2186 mL 1.0932 mL 2.1865 mL 5.4662 mL
15 mM 0.1458 mL 0.7288 mL 1.4576 mL 3.6441 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:

BGB-102807640-87-5JNJ-26483327BGB102BGB 102JNJ26483327JNJ 26483327EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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目录号：
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