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NVP-TAE 226 (Synonyms: TAE226) 纯度: 99.92%
NVP-TAE 226 (TAE226) 是一种有效且具有 ATP 竞争性的双重 FAK 和 IGF-1R 抑制剂,IC50 分别为 5.5 nM、140 nM。NVP-TAE 226 (TAE226) 还有效抑制 Pyk2,胰岛素受体 (InsR),IC50 分为 3.5 nM、40 nM。
NVP-TAE 226 Chemical Structure
CAS No. : 761437-28-9
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1377 | In-stock | |
5 mg | ¥1252 | In-stock | |
10 mg | ¥1989 | In-stock | |
50 mg | ¥7792 | In-stock | |
100 mg | ¥13783 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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NVP-TAE 226 相关产品
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- Endocrinology Compound Library
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- Angiogenesis Related Compound Library
生物活性 |
NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively[1][2]. |
IC50 & Target |
IC50: 5.5 nM (FAK), 3.5 nM (Pyk2), 140 nM (IGF-IR), 40 nM (InsR), 0.16 μM (c-Met), 0.36 μM (KDR), 0.48 μM (Flt3)[1] |
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体外研究 (In Vitro) |
NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC50 range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr395). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G2-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G2-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
468.94 |
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Formula |
C23H25ClN6O3 |
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CAS 号 |
761437-28-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (106.62 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
Glioma cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2×104 in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyzer. The antiproliferative activity of NVP-TAE 226 (ranging from 0.25 to 1 μM) on cells growing in culture is determined using a tetrazolium-based colorimetric MTT assay[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Mice[1] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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