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A 83-01

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A 83-01 是一種有效的 TGF-β I 型受體 ALK5,ALK4 和 ALK7 的抑制劑,能夠抑制 ALK5,ALK4 和 ALK7 誘導(dǎo)的轉(zhuǎn)錄,IC50 值分別為 12 nM,45 nM 和 7.5 nM。貨號:HY-10432
參數(shù)品牌:MCE
產(chǎn)品參數(shù)
品牌:MCE
型號:HY-10432
起訂量:1
規(guī)格::5mg
價格::¥650
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產(chǎn)品詳情

A 83-01 

A 83-01 是一種有效的 TGF-β I 型受體 ALK5ALK4 和 ALK7 的抑制劑,能夠抑制 ALK5,ALK4 和 ALK7 誘導(dǎo)的轉(zhuǎn)錄,IC50 值分別為 12 nM,45 nM 和 7.5 nM。


生物活性

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5ALK4 and ALK7, respectively


體外研究(In Vitro)

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation


體內(nèi)研究(In Vivo)

A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells


分子量:421.52


Formula:C25H19N5S


CAS 號:909910-43-6


運輸條件:Room temperature in continental US; may vary elsewhere.


儲存方式:

-20°C, protect from light, stored under nitrogen

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。


溶解性數(shù)據(jù)


DMSO : 25 mg/mL (59.31 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.3724 mL11.8618 mL23.7237 mL
5 mM0.4745 mL2.3724 mL4.7447 mL
10 mM0.2372 mL1.1862 mL2.3724 mL
*

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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

In Vivo:

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(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)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(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 1.


    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic


  • 2.


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

    Solubility: 1.25 mg/mL (2.97 mM); Clear solution; Need ultrasonic


  • 3.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.97 mM); Clear solution


參考文獻

[1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.

[2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.

[3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.


A 83-01

A 83-01

分享到微信

×
A 83-01 是一種有效的 TGF-β I 型受體 ALK5,ALK4 和 ALK7 的抑制劑,能夠抑制 ALK5,ALK4 和 ALK7 誘導(dǎo)的轉(zhuǎn)錄,IC50 值分別為 12 nM,45 nM 和 7.5 nM。貨號:HY-10432
品牌:MCE
型號:HY-10432
起訂量:1
規(guī)格::5mg
價格::¥650
15906629305
在線客服
產(chǎn)品詳情

A 83-01 

A 83-01 是一種有效的 TGF-β I 型受體 ALK5,ALK4 和 ALK7 的抑制劑,能夠抑制 ALK5,ALK4 和 ALK7 誘導(dǎo)的轉(zhuǎn)錄,IC50 值分別為 12 nM,45 nM 和 7.5 nM。


生物活性

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5ALK4 and ALK7, respectively


體外研究(In Vitro)

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation


體內(nèi)研究(In Vivo)

A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells


分子量:421.52


Formula:C25H19N5S


CAS 號:909910-43-6


運輸條件:Room temperature in continental US; may vary elsewhere.


儲存方式:

-20°C, protect from light, stored under nitrogen

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。


溶解性數(shù)據(jù)


DMSO : 25 mg/mL (59.31 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.3724 mL11.8618 mL23.7237 mL
5 mM0.4745 mL2.3724 mL4.7447 mL
10 mM0.2372 mL1.1862 mL2.3724 mL
*

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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用

In Vivo:

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(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)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(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 1.


    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic


  • 2.


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

    Solubility: 1.25 mg/mL (2.97 mM); Clear solution; Need ultrasonic


  • 3.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.97 mM); Clear solution


參考文獻

[1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.

[2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.

[3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.


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