WHI-P131

SKU: orb1306654

特色

描述

JANEX-1

研究领域

Cell Biology, Immunology & Inflammation, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	202475-60-3
MW	333.78
纯度	>98%
分子式	C₁₆H₁₅N₃O₃ · HCl
SMILES	COc1cc2ncnc(Nc3ccc(O)cc3)c2cc1OC
靶点	Kinase
溶解性	Soluble in DMSO (up to 50 mg/ml).

生物活性

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靶点 IC50	JAK3:78 μM
体内	JANEX-1 is administered in doses from 5 to 100 mg/kg, showing a dose-response relationship with an ED50 of 7.44 mg/kg, significantly reducing CPK and LDH levels in mice. These mice also exhibit a notably smaller infarct size (30.16±2.79%) compared to I/R-operated mice (65.64±3.76%). JANEX-1, also known as WHI-P131, is quickly absorbed, reaching peak plasma concentration in roughly 24.7±1.7 minutes, and has a short elimination half-life of 45.6±5.5 minutes. Despite the maximum plasma concentration being only half of what is observed with intravenous (i.v.) administration at the same dose, intraperitoneal (i.p.) bioavailability stands at 94.6%, with systemic exposure levels (AUC) closely matching those seen after i.v. injection (17.1±2.2 μM·h versus 18.1±1.2 μM·h).
体外	JANEX-1 (WHI-P131) exhibits strong inhibitory activity against JAK3 with an IC50 value of 78 μM, while showing no inhibitory effects on JAK1, JAK2, and various tyrosine kinases including SYK, BTK, LYN, and the insulin receptor kinase, even at concentrations up to 350 μM. It specifically induces apoptosis in human leukemia cell lines expressing JAK3 (NALM-6 and LC1;19) without affecting melanoma (M24-MET) or squamous carcinoma (SQ20B) cells. Furthermore, WHI-P131 effectively suppresses the clonogenic growth of several JAK3-positive leukemia cell lines (DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60) in a concentration-dependent manner, with EC50 values of 24.4 μM and 18.8 μM for NALM-6 and DAUDI cells respectively, achieving more than 99% inhibition of colony formation at 100 μM. However, it does not impede the clonogenic proliferation of JAK3-negative cancer cell lines such as BT-20 breast cancer, M24-MET melanoma, or SQ20B squamous carcinoma.
细胞研究	JANEX-1 (WHI-P131) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use. The following cell lines are used in various biological assays: NALM-6 (pre-B-ALL), LC1;19 (pre-B-ALL), DAUDI (B-ALL), RAMOS (B-ALL), MOLT-3 (T-cell ALL), HL60 (acute myelogenous leukemia), BT-20 (breast cancer), M24-MET (melanoma), SQ20B (squamous cell carcinoma), and PC3 (prostate cancer). These cell lines are maintained in culture. Cells are seeded in six-well tissue culture plates at a density of 50×104 cells/well in a treatment medium containing various concentrations of JANEX-1 (0.1, 0.2, 0.3, 0.4 and 0.5 nM) and incubated for 24-48 h at 37°C in a humidified 5% CO2 atmosphere. Cells are examined for apoptotic changes after treatment with JANEX-1 by the in situ TdT-mediated dUTP end-labeling assay using the ApopTag apoptosis detection kit.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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JANEX-1

相似产品

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Item 1 of 1
WHI-P131 [orb321976]
纯度：
≥99%
CAS 号：
202475-60-3
MW:
333.77
分子式：
C₁₆H₁₅N₃O₃ HCl
可选规格： 50 mg, 250 mg
JANEX-1 hydrochloride [orb2646118]
CAS 号：
188829-39-2
MW:
333.77
分子式：
C₁₆H₁₆ClN₃O₃
可选规格： 25 mg, 100 mg, 50 mg
WHI-P131 [orb1225745]
纯度：
>98% (HPLC)
CAS 号：
202475-60-3
MW:
297.31
分子式：
C₁₆H₁₅N₃O₃
可选规格： 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 500 mg, 1 g

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

3794 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	≥99%
CAS 号：	202475-60-3
MW:	333.77
分子式：	C₁₆H₁₅N₃O₃ HCl

CAS 号：	188829-39-2
MW:	333.77
分子式：	C₁₆H₁₆ClN₃O₃

纯度：	>98% (HPLC)
CAS 号：	202475-60-3
MW:	297.31
分子式：	C₁₆H₁₅N₃O₃

WHI-P131

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

WHI-P131 [orb321976]

JANEX-1 hydrochloride [orb2646118]

WHI-P131 [orb1225745]

质量保证

化合物标识

关键属性

实验方案信息

可选规格