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

RO9021 是一種可口服的,ATP 競爭性的 SYK 抑制劑,IC50 值為 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

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

體外研究
(In Vitro)

RO9021 是一種高選擇性 SYK 抑制劑,S (99) 的 S 分數(shù)低,S (90) 的 S 分數(shù)低,為 0.015,這表明在總共 392 種測試的激酶中,SYK 是唯一與 RO9021 具有 99% 競爭的激酶。RO9021 抑制抗 IgM 誘導的 BTK、PLCγ2、AKT 和 ERK 磷酸化,表明 RO9021 對 SYK 激酶活性的阻斷導致 BCR 下游信號級聯(lián)的減弱。RO9021 選擇性抑制 B 細胞受體信號傳導。RO9021 在 FcεR 介導的肥大細胞活化和脫顆粒試驗中也表現(xiàn)出類似的抑制效力 (IC50=22.8±1.7 nM)[1]

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

分子量

355.44

Formula

C18H25N7O

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 3.03 mg/mL (8.52 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻
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.

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
RO9021
目錄號:
HY-16902
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