2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. JAK STAT Apoptosis
  4. JAK2-IN-14

JAK2-IN-14 是一种口服有效的 JAK2 抑制剂，其 IC50 为 2 nM。JAK2-IN-14 对 JAK1、JAK3 和 TYK2 的选择性是 JAK2 的 89.5 倍、80.5 倍和 51 倍。JAK2-IN-14 抑制 STAT5 信号通路。JAK2-IN-14 可导致肿瘤细胞周期停滞和凋亡 (apoptosis)。JAK2-IN-14 可用于骨髓增生性肿瘤 (MPN) 的研究。

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JAK2-IN-14

JAK2-IN-14 Chemical Structure

CAS No. : 3087335-24-5

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JAK2-IN-14 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK2-IN-14 is an orally active JAK2 inhibitor with an IC50 of 2 nM. JAK2-IN-14 demonstrates 89.5-, 80.5-, and 51-fold selectivity over JAK1, JAK3, and TYK2, respectively. JAK2-IN-14 inhibits STAT5 signaling pathway. JAK2-IN-14 causes tumor cell cycle arrest and apoptosis. JAK2-IN-14 can used for the study of myeloproliferative neoplasms (MPNs)[1].

IC50 & Target[1]

JAK2

2 nM (IC50)

JAK1

179 nM (IC50)

JAK3

161 nM (IC50)

Tyk2

102 nM (IC50)

STAT5

 

体外研究
(In Vitro)

JAK2-IN-14 (Compound 15au) (0.01-5 μM, 24 h) 在 BaF3-JAK2V617F 和 HEL 细胞中以剂量依赖性方式显著诱导细胞周期停滞于 G2/M 期并诱导细胞凋亡[1]。
JAK2-IN-14 (0.05-1 μM, 2 h) 可在 BaF3-JAK2V617F 和 HEL 细胞中有效抑制 JAK2 及其下游信号分子 STAT5 的磷酸化[1]。

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

JAK2-IN-14 相关抗体:

Cell Cycle Analysis[1]

Cell Line: BaF3-JAK2V617F and HEL cells
Concentration: 10, 50, 100, 500 and 1000 nM
Incubation Time: 24 h
Result: Blocked the progression of tumor cells at the G2/M phase, leading to a decrease in the proportions of cells in the G1/G0 and G2 phases.

Western Blot Analysis[1]

Cell Line: BaF3-JAK2V617F and HEL cells
Concentration: 10, 50, 100, 500 and 1000 nM
Incubation Time: 2 h
Result: Reduced p-JAK2 and p-STAT5 levels concentration-dependently.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 5 mg/kg p.o. Cmax 2101.0 ng/mL
Mice 5 mg/kg p.o. Tmax 1.0 h
Mice 5 mg/kg p.o. T1/2 7.8 h
Mice 5 mg/kg p.o. CL/F 1.0 L/h/kg
Mice 5 mg/kg p.o. AUC0-t 5069.7 ng·h/mL
体内研究
(In Vivo)

JAK2-IN-14 (Compound 15au) (7.5-40 mg/kg, p.o., 每日一次共 13-28 天) 显著抑制 BaF3-JAK2V617F 和 HEL 细胞异种移植小鼠模型中的肿瘤生长[1]。

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

Animal Model: BaF3-JAK2V617F allogeneic transplantation model established in BALB/c-nude mice[1]
Dosage: 7.5, 15 and 30 mg/kg
Administration: Oral administration (p.o.), once daily for 13 days
Result: Demonstrated significant therapeutic efficacy, reducing spleen weight by 24.1%, 26.4%, and 40.5% at doses of 7.5, 15, and 30 mg/kg, respectively
Animal Model: HEL cells xenograft model was established in 6-week-old male BALB/c nude mice[1]
Dosage: 20 and 40 mg/kg
Administration: Oral administration (p.o.), once daily for 28 days
Result: Significantly inhibited subcutaneous tumor growth.
did not induce observable body weight loss during the experimental period.
分子量

459.59

Formula

C26H33N7O
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

JAK2-IN-14 相关分类

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  • 稀释计算器

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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:

JAK2-IN-143087335-24-5JAKSTATApoptosisJanus kinasePharmacokinetic propertiesmacrocyclizationkinase selectivityBaF3-JAK2V617FHEL cellsInhibitorinhibitorinhibit

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