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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-GDC-046
GDC-046

Chemical Structure : GDC-046

CAS No.: 1258292-64-6

GDC-046 (GDC046)

货号: PC-38049Not For Human Use, Lab Use Only.

GDC-046 is a potent, selective, and orally bioavailable inhibitor of TYK2 with  with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

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10 mg ¥1480 In stock
25 mg ¥2580 In stock
50 mg ¥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-046 is a potent, selective, and orally bioavailable inhibitor of TYK2 with  with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) in cell based assays.
GDC-046 also displays less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM), and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM).
GDC-046 shows statistically significant knockdown of cytokine interferon-γ (IFNγ), in a mouse IL-12 PK/PD model.

物理化学性质&存储条件

分子量 350.199
分子式 C16H13Cl2N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

参考文献

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