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  2. Protein Tyrosine Kinase/RTK Autophagy
  3. Src Bcr-Abl Autophagy
  4. Bosutinib

Bosutinib  (Synonyms: 博舒替尼; SKI-606)

目錄號: HY-10158 純度: 99.89%
COA 產品使用指南

Bosutinib是一種口服 Src/Abl 酪氨酸激酶抑制劑，IC50 分別為 1.2 nM 和1 nM。

MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務

Bosutinib Chemical Structure

Bosutinib Chemical Structure

CAS No. : 380843-75-4

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規(guī)格 價格 是否有貨 數量
10 mM * 1 mL in DMSO ￥500
In-stock
1 mg ￥140
In-stock
5 mg ￥281
In-stock
10 mg ￥450
In-stock
50 mg ￥850
In-stock
100 mg ￥1100
In-stock
200 mg ￥1800
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Bosutinib:

查看 Src 亞型特異性產品:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

生物活性

Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively[1].

IC50 & Target

IC50: 1.2 nM (Src), 1 nM (Abl)[1]
細胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 10 μM
Compound: SKI-606
Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay
Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay
[PMID: 16970400]
BaF3 IC50
> 20 μM
Compound: SKI-606
Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay
Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay
[PMID: 16970400]
BaF3 IC50
0.15 μM
Compound: SKI-606
Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay
Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay
[PMID: 16970400]
BaF3 IC50
0.2 μM
Compound: SKI-606
Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay
Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay
[PMID: 16970400]
BaF3 IC50
0.2 μM
Compound: SKI-606
Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay
Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay
[PMID: 16970400]
BaF3 IC50
1 μM
Compound: SKI-606
Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay
Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay
[PMID: 16970400]
BaF3 IC50
3.2 μM
Compound: Bosutinib
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
[PMID: 26814890]
Fibroblast IC50
100 nM
Compound: 1a
Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA
Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA
[PMID: 17905586]
HeLa IC50
3.85 μM
Compound: Bosutinib
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
HepG2 GI50
1.15 μM
Compound: bosutinib, SKI-606
Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay
[PMID: 18485715]
HepG2 IC50
3.91 μM
Compound: bosutinib, SKI-606
Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay
[PMID: 18485715]
HT-29 GI50
1.17 μM
Compound: bosutinib, SKI-606
Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay
[PMID: 18485715]
HT-29 IC50
3.87 μM
Compound: bosutinib, SKI-606
Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay
[PMID: 18485715]
K562 IC50
0.0043 μM
Compound: Bosutinib
Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 26814890]
體外研究
(In Vitro)

博舒替尼 (SKI-606) 是多種慢性粒細胞白血病細胞系中 Bcr-Abl 的活性抑制劑，其 IC50 值在低納摩爾范圍內[2]。

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

Cell Proliferation Assay[2]

Cell Line: The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)
Concentration: 0.1 μmol/L
Incubation Time: 72 h
Result: Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L
體內研究
(In Vivo)

Fasudil Hydrochloride（口服管飼；75 mg/kg，每日兩次或 150 mg/kg，每日一次）對裸鼠中的人類 KU812 異種移植瘤有活性。Fasudil Hydrochloride（150 mg/kg；每日一次，每周 5 天）對同源 Bcr-Abl WT 和突變體有活性Ba/F3 異種移植[2]。

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

Animal Model: KU812CM L xenograft model[2]
Dosage: 75 mg/kg twice daily or 150 mg/kg once daily
Administration: Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily)
Result: Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.
Animal Model: Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2]
Dosage: 150 mg/kg
Administration: Bosutinib (150 mg/kg; once daily, 5 days weekly)
Result: Decreased the rate of tumor growth and prolonged event-free survival of mice.
Clinical Trial
分子量

530.45

Formula

C26H29Cl2N5O3
CAS 號
性狀

固體

顏色

White to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

溶解性數據
細胞實驗： 

DMSO 中的溶解度 : ≥ 46 mg/mL (86.72 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 1.8852 mL 9.4260 mL 18.8519 mL
5 mM 0.3770 mL 1.8852 mL 3.7704 mL
查看完整儲備液配制表

* 請根據產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品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內使用， -20°C儲存時，請在6個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
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

動物實驗：

請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.71 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

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

動物數量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網站選購。 ，Tween 80，均可在 MCE 網站選購。
計算結果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。
動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產品資料

純度: 99.96%

參考文獻

完整儲備液配制表

* 請根據產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品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內使用， -20°C儲存時，請在6個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8852 mL 9.4260 mL 18.8519 mL 47.1298 mL
5 mM 0.3770 mL 1.8852 mL 3.7704 mL 9.4260 mL
10 mM 0.1885 mL 0.9426 mL 1.8852 mL 4.7130 mL
15 mM 0.1257 mL 0.6284 mL 1.2568 mL 3.1420 mL
20 mM 0.0943 mL 0.4713 mL 0.9426 mL 2.3565 mL
25 mM 0.0754 mL 0.3770 mL 0.7541 mL 1.8852 mL
30 mM 0.0628 mL 0.3142 mL 0.6284 mL 1.5710 mL
40 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1782 mL
50 mM 0.0377 mL 0.1885 mL 0.3770 mL 0.9426 mL
60 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7855 mL
80 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5891 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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