1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. RO9021

RO9021 是一种可口服的,ATP 竞争性的 SYK 抑制剂,IC50 值为 5.6 nM。

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RO9021 Chemical Structure

RO9021 Chemical Structure

CAS No. : 1446790-62-0

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.

IC50 & Target

IC50: 5.6 nM (SYK)

体外研究
(In Vitro)

RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay[1].

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

分子量

355.44

Formula

C18H25N7O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 3.03 mg/mL (8.52 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8134 mL 14.0671 mL 28.1341 mL
5 mM 0.5627 mL 2.8134 mL 5.6268 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Kinase Assay
[1]

The inhibitory potency to SYK is determined in a radiometric assay using inactive SYK kinase. Briefly, SYK protein is dephosphorylated by PTP1B phosphatase and then the reaction is initiated by the addition of substrate cocktail that contained 20 μM ATP, 0.025 μCi ATP-γ-33P and 10 μM biotinylated synthetic peptide. The reaction is carried out for 30 minutes and resulting 33P incorporation is determined by top counter.

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

Animal Administration
[1]

Briefly, DBA1/J male mice are injected intradermally with 0.1 mL bovine type II collagen (100 μg) and complete Freund’s adjuvant followed by second immunization on day 21 with bovine type II collagen and incomplete Freund adjuvant. RO9021 is administered orally, randomized into different groups (14 mice/groups), every day for 14 days starting on the day after second immunization. Clinical arthritis scores (1 to 4) of individual paws are assessed and the arthritic index for each mouse is determined by adding the individual scores of all four paws. The level of cytokines in serum is determined by Luminex analysis.

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8134 mL 14.0671 mL 28.1341 mL 70.3354 mL
5 mM 0.5627 mL 2.8134 mL 5.6268 mL 14.0671 mL
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.

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Inquiry Information

产品名称:
RO9021
目录号:
HY-16902
需求量: