2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK STAT
  4. JAK2-IN-13

JAK2-IN-13 是一种强效且口服有效的 JAK2 抑制剂，其 IC50 为 54.7 nM。JAK2-IN-13 可下调 p-STAT3 和 p-STAT5 的表达。JAK2-IN-13 具有良好的生物利用度，并能有效抑制重组人促红细胞生成素诱导的髓外红细胞生成以及真性红细胞增多症。JAK2-IN-13 可用于骨髓增生性肿瘤的研究。

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JAK2-IN-13

JAK2-IN-13 Chemical Structure

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JAK2-IN-13 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:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expressions of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms[1].

IC50 & Target[1]

JAK2

54.7 nM (IC50)

STAT3

 

STAT5

 

体外研究
(In Vitro)

JAK2-IN-13 (Compound 11) (0.011-25 μM, 72 h) 对 HEL 和 SET-2 细胞显示出强效的抑制活性，IC50 值分别为 0.57 μM 和 1.07 μM[1]。
JAK2-IN-13 (0-10 μM, 3 h) 在 HEL 细胞中显著抑制 JAK2 下游信号通路，并下调 p-STAT3 和 p-STAT5 的表达[1]。

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

JAK2-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: HEL cells
Concentration: 0, 0.3, 1, 5, 10 μM
Incubation Time: 3 h
Result: Dose-dependent downregulated p-STAT3 and p-STAT5 expressions.
Significantly inhibited the phosphorylation of STAT3 and STAT5 at 10 μM for 4 h.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 4.59 h
Mice 5 mg/kg p.o. F 54.8 %
Mice 1 mg/kg i.v. Tmax 2 h
Mice 5 mg/kg p.o. T1/2 4.07 h
Mice 1 mg/kg i.v. Cmax 29.23 ng/mL
Mice 5 mg/kg p.o. Tmax 6 h
Mice 1 mg/kg i.v. AUCinf 166.95 ng·h/mL
Mice 5 mg/kg p.o. Cmax 42.7 ng/mL
Mice 5 mg/kg p.o. AUCinf 457.38 ng·h/mL
体内研究
(In Vivo)

JAK2-IN-13 (Compound 11) (50-100 mg/kg, p.o., 每日 1 次，连用 4 天) 在 rhepo 诱导的红细胞增多症模型抑制了髓外红细胞生成和真性红细胞增多症[1]。

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

Animal Model: rhEPO-induced polycythemia model established in female BALB/c mice (8−10 weeks, 17−20 g)[1]
Dosage: 50, 75 and 100 mg/kg
Administration: Oral administration (p.o.), once daily for 4 days
Result: Suppressed the increase in reticulocyte counts and hematocrit expansion induced by rhEPO and alleviated splenomegaly.
Inhibited the expansion of Ter119/CD71 erythroblasts in both the spleen and bone marrow.
Had no significant impact on white blood cell counts and body weight.
分子量

465.98

Formula

C25H28ClN5O2
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-13 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-13JAKSTATJanus kinaseMyeloproliferative neoplasmsHEL cellsSET-2 cellsBALB/c miceInhibitorinhibitorinhibit

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