A-770041是一种选择性 Src 家族激酶 Lck 的抑制剂,对 Lck(1 mM ATP)的 IC50 为 147 nM,相对 Fyn 的选择性高达 300 倍,可用于急性排斥反应研究。


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| 产品名称 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
| SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
| PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
| PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
| WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
| NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
| CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
| MNS |
+
Src, IC50: 29.3 μM |
Syk,p97 | 98% | ||||||||||||||||
| Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
| PP121 |
++
Src, IC50: 14 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Quercetin | ✔ | Sirtuin,PKC | 95% | ||||||||||||||||
| Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Repotrectinib |
+++
Src, IC50: 5.3 nM |
99% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | A-770041 is selective and orally active Src-family Lck inhibitor and is a 147 nM inhibitor of Lck(1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling. |
| Concentration | Treated Time | Description | References | |
| XF354 cells | 500 nM | 24 h | Inhibition of LCK activity, reducing cell migration | Mol Cancer. 2021 Jun 11;20(1):88 |
| SAS cells | 500 nM | 24 h | Inhibition of LCK activity, reducing cell migration and invasion | Mol Cancer. 2021 Jun 11;20(1):88 |
| KHOS R2 | 0.5 μM | 96 h | Increased drug sensitivities to paclitaxel and doxorubicin and reversed drug resistance | BMC Cancer. 2014 Sep 19;14:681 |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | Cockroach extract (CE)-induced allergic asthma model | Intranasally (i.n.) | 10 mg/kg | For 5 consecutive days, 30 min before CE challenge (day 11–15) | To assess the effect of LCK inhibitor A-770041 on allergic airway inflammation, results showed that A-770041 significantly reduced airway inflammation and mucus secretion, and decreased the expression of Th2-related cytokines (IL-4/IL-5/IL-13). | Metabolites. 2022 Aug 25;12(9):793 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.61mL 0.32mL 0.16mL |
8.04mL 1.61mL 0.80mL |
16.08mL 3.22mL 1.61mL |
|
| CAS号 | 869748-10-7 |
| 分子式 | C34H39N9O3 |
| 分子量 | 621.73 |
| SMILES Code | NC1=C2C(N([C@@H]3CC[C@@H](N4CCN(C(C)=O)CC4)CC3)N=C2C5=CC=C(NC(C6=CC7=C(C=CC=C7)N6C)=O)C(OC)=C5)=NC=N1 |
| MDL No. | MFCD24873124 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 25 mg/mL(40.21 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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