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 (tautomerism)

Rafutrombopag (tautomerism)  (Synonyms: 海曲泊帕; Hetrombopag (tautomerism); SHR-8735 (tautomerism))

目录号: HY-122620 纯度: 98.33%
COA 产品使用指南 技术支持

Rafutrombopag (tautomerism) (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[1][2][3]。

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Rafutrombopag (tautomerism)

Rafutrombopag (tautomerism) Chemical Structure

CAS No. : 2114365-78-3

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Other Forms of Rafutrombopag (tautomerism):

Rafutrombopag (tautomerism) 相关抗体

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

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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 (tautomerism) (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 (tautomerism) 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: human UCB MNCs
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
性状

固体

颜色

Brown to reddish brown

中文名称

海曲泊帕
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 : 10 mg/mL (21.81 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)

DMF 中的溶解度 : 6.25 mg/mL (13.63 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1812 mL 10.9058 mL 21.8117 mL
5 mM 0.4362 mL 2.1812 mL 4.3623 mL
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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。

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纯度 & 产品资料

纯度: 98.33%

COA (289 KB) HNMR (291 KB) LCMS (90 KB)

产品使用指南 (1538 KB)
参考文献

Rafutrombopag (tautomerism) 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
DMF / DMSO 1 mM 2.1812 mL 10.9058 mL 21.8117 mL 54.5292 mL
5 mM 0.4362 mL 2.1812 mL 4.3623 mL 10.9058 mL
10 mM 0.2181 mL 1.0906 mL 2.1812 mL 5.4529 mL
DMSO 15 mM 0.1454 mL 0.7271 mL 1.4541 mL 3.6353 mL
20 mM 0.1091 mL 0.5453 mL 1.0906 mL 2.7265 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:

Rafutrombopag (tautomerism)2114365-78-3Hetrombopag (tautomerism)SHR-8735 (tautomerism)海曲泊帕Thrombopoietin ReceptorSTATPI3KERKApoptosisCDKPhosphoinositide 3-kinaseExtracellular signal regulated kinasesCyclin dependent kinaseEltrombopagHetrombopagHollow-fibre assayThrombopoietinThrombopoietin receptorHSC/HPCsCardiac myocyte viabilityOxidative stressInhibitorinhibitorinhibit

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