2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK
  3. Aurora Kinase FGFR VEGFR
  4. Tinengotinib

Tinengotinib  (Synonyms: TT 00420)

目录号: HY-145601 纯度: 99.57%
COA 产品使用指南 技术支持

Tinengotinib (TT 00420) 是一种口服有效、光谱选择性小分子激酶抑制剂，靶向 Aurora A/B (IC50=1.2-3.3 nM)、FGFR1/2/3 (IC50=1.5-3.5 nM)、VEGFRs、JAK1/2 及 CSF1R 等。Tinengotinib 阻断 Aurora 激酶介导的细胞周期进程 (诱导 G2/M 期阻滞)、抑制 FGFR/JNK-JUN 信号通路及激活 MEK/ERK 依赖的凋亡途径。Tinengotinib 具有抗肿瘤增殖、诱导凋亡 (apoptosis)、抑制血管生成及调节肿瘤微环境的活性。Tinengotinib 可用于三阴性乳腺癌 (TNBC)、胆囊癌、肿瘤免疫微环境的研究。

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Tinengotinib Chemical Structure

Tinengotinib Chemical Structure

CAS No. : 2230490-29-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1496
In-stock
5 mg ￥1360
In-stock
10 mg ￥2000
In-stock
25 mg ￥3400
In-stock
50 mg ￥4800
In-stock
100 mg 现货 询价
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500 mg   询价  

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Customer Review

Tinengotinib 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment[1][2].

IC50 & Target

FGFR1

 

FGFR2

 

FGFR3

 

Aurora A

 

Aurora B

 

体外研究
(In Vitro)

Tinengotinib (0.1-10 μM；72 h) 呈浓度依赖性抑制三阴性乳腺癌 (TNBC) 细胞系 (MDA-MB-468、HCC1806) 及胆囊癌细胞系 (NOZ、GBC-SD) 的细胞增殖，诱导 G2/M 期细胞周期阻滞及凋亡，并下调 Aurora A/B、FGFR1/2/3 及 JNK/JUN 信号通路相关蛋白表达[1]。
Tinengotinib (1 μM；48 h) 抑制人脐静脉内皮细胞 (HUVEC) 细胞中 VEGFR2 磷酸化，减少血管生成相关蛋白表达，抑制体外血管形成[1]。

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

Tinengotinib 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-468, HCC1806 (TNBC); NOZ, GBC-SD (gallbladder cancer)
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 72 hours
Result: Significantly reduced cell viability in a dose-dependent manner, with IC50 values of 0.73 μM (MDA-MB-468), 0.42 μM (HCC1806), 0.076 μM (NOZ), and 0.18 μM (GBC-SD).
Resulted a 60-80% reduction in colony number at 5 μM compared to control.
体内研究
(In Vivo)

Tinengotinib (15 mg/kg；口服灌胃；每日 1 次；2-3 周) 在裸鼠三阴性乳腺癌 (HCC1806) 皮下移植瘤模型及 NOZ 胆囊癌皮下移植瘤模型中显著抑制肿瘤生长，降低肿瘤重量及增殖标志物 Ki67 表达[1][2]。
Tinengotinib (15 mg/kg；口服灌胃；每日 1 次；4 周) 减少患者来源的胆囊癌异种移植 (PDX) 小鼠模型的肿瘤体积，抑制血管生成标志物 CD34 表达[2]。

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

Animal Model: BALB/c nude mice (female, 20-22 g, 6 weeks old) with subcutaneous HCC1806 triple-negative breast cancer (TNBC) xenografts[1]
Dosage: 15 mg/kg
Administration: Oral gavage, daily, for 2-3 weeks
Result: Significantly inhibited tumor growth, with a dose-dependent reduction in tumor volume and weight.
Downregulated the proliferation marker Ki67 in tumor tissues in Immunohistochemistry (IHC) staining assay.
Showed a rapid distribution to tumor sites, with peak concentrations at 7 hours post-dosing and no significant systemic toxicity observed in Pharmacokinetic analysis.
Animal Model: BALB/c nude mice (male, 25-30 g, 6 weeks old) with patient-derived gallbladder cancer (GBC) xenografts (PDX)[2]
Dosage: 15 mg/kg
Administration: Oral gavage, daily, for 4 weeks
Result: Led to a significant decrease in tumor volume and weight compared to the control group.
Reduced expression of the angiogenesis marker CD34, suggesting inhibition of tumor vascularization in IHC staining assay.
No significant changes in mouse body weight or organ toxicity were observed during the treatment period.
Clinical Trial
分子量

394.86

Formula

C20H19ClN6O
CAS 号
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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (126.63 mM; 超声助溶 (<60°C); 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 2.5325 mL 12.6627 mL 25.3254 mL
5 mM 0.5065 mL 2.5325 mL 5.0651 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

纯度: 99.57%

COA (295 KB) HNMR (277 KB) LCMS (96 KB)

产品使用指南 (1538 KB)
参考文献

Tinengotinib 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 2.5325 mL 12.6627 mL 25.3254 mL 63.3136 mL
5 mM 0.5065 mL 2.5325 mL 5.0651 mL 12.6627 mL
10 mM 0.2533 mL 1.2663 mL 2.5325 mL 6.3314 mL
15 mM 0.1688 mL 0.8442 mL 1.6884 mL 4.2209 mL
20 mM 0.1266 mL 0.6331 mL 1.2663 mL 3.1657 mL
25 mM 0.1013 mL 0.5065 mL 1.0130 mL 2.5325 mL
30 mM 0.0844 mL 0.4221 mL 0.8442 mL 2.1105 mL
40 mM 0.0633 mL 0.3166 mL 0.6331 mL 1.5828 mL
50 mM 0.0507 mL 0.2533 mL 0.5065 mL 1.2663 mL
60 mM 0.0422 mL 0.2110 mL 0.4221 mL 1.0552 mL
80 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
100 mM 0.0253 mL 0.1266 mL 0.2533 mL 0.6331 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:

Tinengotinib2230490-29-4TT 00420TT00420TT-00420Aurora KinaseFGFRVEGFRFibroblast growth factor receptorVascular endothelial growth factor receptorAuroraanti-cancerInhibitorinhibitorinhibit

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