2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. H3B-6527

H3B-6527 是一种具有口服活性的，高选择性和共价 FGFR4 抑制剂，IC50 <1.2 nM。H3B-6527 抑制 FGFR1-3，IC50 分别为 320、1290 和 1060 nM。H3B-6527 具有良好的抗癌活性。

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H3B-6527 Chemical Structure

H3B-6527 Chemical Structure

CAS No. : 1702259-66-2

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1 mg ￥800
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5 mg ￥2100
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10 mg ￥3600
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Customer Review

H3B-6527 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity[1].

IC50 & Target[1]

FGFR4

<1.2 nM (IC50)

FGFR1

320 nM (IC50)

FGFR2

1290 nM (IC50)

FGFR3

1060 nM (IC50)

体外研究
(In Vitro)

H3B-6527 inhibits TAOK2, JNK2, and CSF1R with IC50s of 690 nM, >10000 nM, and >10000 nM, respectively[1].
H3B-6527 (10-10000 nM; 72 hours) results in a GI50 value of 25 nM[1].
H3B-6527 (10-10000 nM; 72 hours) leads cell death in HCC cell lines[1].
H3B-6527 (0.1-1000 nM; 1 hour) decreases the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM[1].
H3B-6527 (1-1000 nM; 24 hours) causes a robust increase in CYP7A1 transcripts[1].

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

H3B-6527 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 72 hours
Result: Resulted in a GI50 value of 25 nM.

Apoptosis Analysis[1]

Cell Line: Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 72 hours
Result: Leaded cell death in HCC cell lines.

Western Blot Analysis[1]

Cell Line: Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration: 0.1, 0.3, 1, 3, 10, 100, 1000 nM
Incubation Time: 1 hour
Result: Decreased the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM.

RT-PCR[1]

Cell Line: Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 hours
Result: Caused a robust increase in CYP7A1 transcripts.
体内研究
(In Vivo)

H3B-6527 (10-300 mg/kg; orally; twice-daily; for 15 days) significantly inhibits tumor growth at the 300 and 100 mg/kg and does not inhibit tumor growth at 30 and 10 mg/kg[1].

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

Animal Model: BALB/c nu/nu female mice approximately 8-week-old, weighing 18-20 g bearing Hep3B orthotopic xenografts in liver[1]
Dosage: 10, 30, 100, 300 mg/kg
Administration: Orally; twice-daily; for 15 days
Result: Inhibited tumor growth at the 300 and 100 mg/kg twice-daily dose.
分子量

629.54

Formula

C29H34Cl2N8O4
CAS 号
性状

固体

颜色

White to khaki

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： 

DMSO 中的溶解度 : 2.5 mg/mL (3.97 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 1.5885 mL 7.9423 mL 15.8846 mL
5 mM --- --- ---
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

纯度: ≥98.0%

COA (286 KB) HNMR (281 KB)

产品使用指南 (1538 KB)
参考文献

H3B-6527 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 1.5885 mL 7.9423 mL 15.8846 mL 39.7115 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:

H3B-65271702259-66-2FGFRFibroblast growth factor receptorOrallycovalentanti-cancerTAOK2JNK2CSF1RHepatocellularcarcinomaInhibitorinhibitorinhibit

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