420099

JAK抑制剂I

Name: JAK抑制剂I
Brand: MM

≥98% (HPLC), solid, JAK inhibitor, Calbiochem^®

别名:

Janus蛋白酪氨酸激酶(JAK)抑制剂I, 2-（1，1-二甲基乙基）-9-氟-3，6-二氢-7H-苯并[h]-咪唑[4，5-f]异喹啉-7-酮，吡啶酮6，P6，DBI，JAK1抑制剂I，JAK2抑制剂I，JAK3抑制剂X

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关于此项目

经验公式（希尔记法）:

C₁₈H₁₆FN₃O

化学文摘社编号:

457081-03-7

分子量:

309.34

MDL number:

MFCD17019334

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze
protect from light

主要文件

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产品名称

JAK抑制剂I, JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (K_i= 5 nM) and Tyk2 (IC₅₀ = 1 nM).

SMILES string

Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1

InChI

1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)

InChI key

VNDWQCSOSCCWIP-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
protect from light

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

color

off-white to light brown

Biochem/physiol Actions

主要靶标
鼠JAK1

产物与ATP竞争。

可逆性：是

细胞可渗透性：是

靶标IC₅₀：15 nM，针对鼠JAK1；1 nM，针对JAK2；1 nM，针对Tyk2

靶标K_i：5 nM，针对JAK3

Disclaimer

毒性：标准处理（A）

General description

一种有效、可逆、细胞可渗透和ATP竞争性的Janus蛋白酪氨酸激酶（JAKs）抑制剂。显示对JAK1（对于鼠JAK1，IC₅₀=15 nM）、JAK2（IC₅₀=1 nM）、JAK3（K_i=5 nM）和Tyk2（IC₅₀=1 nM）的有效抑制活性。在高得多的浓度下抑制其他激酶。显示抑制IL2和IL4依赖性的CTLL细胞增殖，并阻断STAT5的磷酸化；并且与AG 490（目录编号658401）不同，进一步诱导表达活化的JAKs和STAT3的多发性骨髓瘤细胞的生长抑制。也可获得10 mM（500 µg/162 µl）JAK抑制剂I的DMSO溶液（目录号420097）。

一种有效、细胞可渗透、可逆和ATP竞争性的Janus蛋白酪氨酸激酶（JAKs）抑制剂。显示对JAK1（对于鼠JAK1，IC₅₀=15 nM）、JAK2（IC₅₀=1 nM）、JAK3（K_i=5 nM）和Tyk2（IC₅₀=1 nM）的有效抑制活性。在高得多的浓度下抑制其他激酶。显示抑制IL2和IL4依赖性的CTLL细胞增殖，并阻断STAT5的磷酸化；并且与AG 490（目录编号658401）不同，进一步诱导表达活化的JAKs和STAT3的多发性骨髓瘤细胞的生长抑制。

Other Notes

Pedranzini, L., et al. 2006.Cancer Res.66, 9714.
Lucet, I.S., et al. 2005.Blood107, 176.
Thompson, J.E., et al. 2002.Bioorg.Med. Chem. Lett.12, 1219.

Packaging

用惰性气体包装

Preparation Note

复溶后，等分并冷冻（-20°C）。储备溶液在-20°C下可稳定保存至多3个月。

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

分析证书(COA)

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M2-polarization and the tumoricidal to tumor-promoting transition are commonly observed with tumor-infiltrating macrophages after interplay with cancer cells or/and other stroma cells. Our previous study indicated that macrophage M2-polarization can be induced by extracellular HSP90α (eHSP90α) secreted from endothelial-to-mesenchymal transition-derived

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JAK抑制剂I

≥98% (HPLC), solid, JAK inhibitor, Calbiochem^®

选择尺寸

关于此项目

主要文件

属性

产品名称

SMILES string

InChI

InChI key

assay

form

manufacturer/tradename

storage condition

solubility

shipped in

storage temp.

Quality Level

color

相关类别

说明

Biochem/physiol Actions

Disclaimer

General description

Other Notes

Packaging

Preparation Note

Legal Information

安全信息

存储类别

wgk

flash_point_f

flash_point_c

文件

分析证书(COA)

已有该产品？

同行评审论文

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相关内容

技术服务

JAK抑制剂I

≥98% (HPLC), solid, JAK inhibitor, Calbiochem®

选择尺寸

关于此项目

主要文件

属性

产品名称

SMILES string

InChI

InChI key

assay

form

manufacturer/tradename

storage condition

solubility

shipped in

storage temp.

Quality Level

color

相关类别

说明

Biochem/physiol Actions

Disclaimer

General description

Other Notes

Packaging

Preparation Note

Legal Information

安全信息

存储类别

wgk

flash_point_f

flash_point_c

文件

分析证书(COA)

已有该产品？

同行评审论文

技术文章和实验方案

相关内容

技术服务

≥98% (HPLC), solid, JAK inhibitor, Calbiochem^®