2. Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis Cell Cycle/DNA Damage
  3. Thrombopoietin Receptor STAT PI3K ERK Apoptosis CDK
  4. Rafutrombopag

Rafutrombopag  (Synonyms: Hetrombopag; SHR-8735)

目录号: HY-145589
产品使用指南 技术支持

Rafutrombopag (Hetrombopag) 是一种口服有效的非肽血小板生成素受体 (TPOR/MPL) 激动剂。 Rafutrombopag 在促进造血的同时，可螯合铁，缓解铁超载。Rafutrombopag 通过刺激 STAT、PI3K 和 ERK 信号通路特异性地刺激人 TPOR-表达细胞 (包括 32D-MPL 和人类造血干细胞) 的增殖和分化。Rafutrombopag 通过调节 32D-MPL 细胞 BCL-XL/BAK 的表达，有效上调 G1 期相关蛋白，包括 p-RB、Cyclin D1 和 CDK4/6，使细胞周期进程正常化，预防细胞凋亡 (apoptosis)。Rafutrombopag 作为干细胞的增强剂，可保护心肌细胞免受氧化应激损伤。 Rafutrombopag 可用于免疫性血小板减少症和氧化应激相关心血管疾病的研究。

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Rafutrombopag

Rafutrombopag Chemical Structure

CAS No. : 2600513-51-5

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Rafutrombopag 的其他形式现货产品:

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Rafutrombopag 相关抗体

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STAT3 STAT5 STAT6 STAT1

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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ERK ERK1 ERK2 ERK5 ERK8

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease[1][2][3].

IC50 & Target[1]

CDK4

 

CDK6

 

PI3K

 

体外研究
(In Vitro)

Rafutrombopag (0.01-1000 nM, 0-7 days) 可刺激细胞内 TPO 信号通路，并以 TPOR 依赖的方式促进 32D-MPL (EC50 = 0.4 nM) 和 BaF3/h TPOP (EC50 = 1.2 nM) 细胞增殖[1][2]。
Rafutrombopag (0.01-10 μM, 0-10 days) 可促进人脐带血来源的 CD34+ 细胞的增殖 (EC50 = 2.3 nM) 和分化[1][2]。
Rafutrombopag (0-3 μM, 24-72 h) 可使 32D-MPL 细胞和大鼠心肌细胞的细胞周期进程正常化，并防止细胞凋亡[1]。
Rafutrombopag (0.01-1000 nM, 30 min-72 h) 可与 TPOR 特异性结合，并与 rhTPO 产生叠加的激动效应[1]。
Rafutrombopag (0.3-3 μM, 12 h) 可通过提高人脐血单个核细胞的活力和增加旁分泌因子的分泌，增强人脐血单个核细胞在氧自由基应激期间受损心肌细胞存活率的有益作用[2]。
Rafutrombopag (3-30 μM) 具有抗炎活性，可显著减少 LPS (HY-D1056) 刺激下的巨噬细胞 RAW264.7 细胞中 NO 和 TNF-a 的产生[2]。

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

Rafutrombopag 相关抗体:

Cell Cycle Analysis[1]

Cell Line: 32D-MPL cells
Concentration: 0.3.1 and 3 nM
Incubation Time: 24 h
Result: Caused cells to re-enter the cell cycle, increasing the proportion of cells in G2 and S phases and decreasing the proportion of cells in G1 phase.
Reversed the decrease in G1-phase-related proteins, including p-RB, Cyclin D and CDK4/6, induced by cytokine withdrawal.

Apoptosis Analysis[1]

Cell Line: 32D-MPL cells
Concentration: 0.3.1 and 3 nM
Incubation Time: 72 h
Result: Reduced the apoptosis effect.
Increased expression of the antiapoptotic family members BCL-XL and MCL-1, and decreased expression of proapoptotic BAK.

Western Blot Analysis[1]

Cell Line: 32D-MPL cells
Concentration: 0.1, 1, 3, 10, 30, 100 nM
Incubation Time: 0, 0.5, 1, 2, 4, 8, 12, 24h
Result: Induced phosphorylation of the major components of TPO‐mediated signalling, including STAT3, STAT5, ERK1/2, and AKT.
Stimulated the phosphorylation of these TPOR downstream effectors in a concentration-dependent manner.

Cell Viability Assay[2]

Cell Line: 32D-MPL cells
Concentration: 0.3.1 and 3 μM
Incubation Time: 12 h
Result: Increased myocyte viability by 20.3%, 43.7% and 46.8% at 0.3, 1 and 3 μM, respectively.
Showed weak antioxidant activity, and increased the myocyte viability by 15.7%.
体内研究
(In Vivo)

Rafutrombopag (18 mg/kg, p.o., 单剂量) 在小鼠中 3 小时时血浆浓度达到峰值 687 ng/mL，24 小时时降至 4.5 ng/mL，STAT3、STAT5 和 ERK1/2 的磷酸化在 3 小时时首次检测到，在 6-12 小时达到峰值，并持续至 24 小时[1]。
Rafutrombopag (18 mg/kg, p.o., 每日一次，连续 12 天) 以时间依赖性方式显著刺激小鼠中空纤维内 32D-MPL 细胞的增殖并防止其凋亡[1]。

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

Animal Model: 32D-MPL cell-containing hollow fibres assay established in mice[1]
Dosage: 18 mg/kg
Administration: Oral administration (p.o.), once daily for 12 days
Result: Significantly stimulated proliferation and prevented apoptosis of 32D-MPL cells in hollow fibres in a time-dependent manner.
Reached the number of 32D-MPL cells a maximum after 3 days and then decreased within 12 days.
Had no effect on the counts of white blood cells, reticulocytes, or platelets in the peripheral blood.
Clinical Trial
分子量

458.47

Formula

C25H22N4O5
CAS 号
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.
纯度 & 产品资料
参考文献

Rafutrombopag 相关分类

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  • 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:

Rafutrombopag2600513-51-5Hetrombopag SHR-8735SHR8735SHR 8735SHR-8735Thrombopoietin ReceptorSTATPI3KERKApoptosisCDKPhosphoinositide 3-kinaseExtracellular signal regulated kinasesCyclin dependent kinaseEltrombopagHollow-fibre assayThrombopoietinThrombopoietin receptorHSC/HPCsCardiac myocyte viabilityOxidative stressInhibitorinhibitorinhibit

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