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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。
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 ALK5, ALK4 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)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.3724 mL | 11.8618 mL | 23.7237 mL |
5 mM | 0.4745 mL | 2.3724 mL | 4.7447 mL |
10 mM | 0.2372 mL | 1.1862 mL | 2.3724 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。
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
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
參考文獻
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 ALK5, ALK4 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)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.3724 mL | 11.8618 mL | 23.7237 mL |
5 mM | 0.4745 mL | 2.3724 mL | 4.7447 mL |
10 mM | 0.2372 mL | 1.1862 mL | 2.3724 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。
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
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
參考文獻