XRP44X 抑制Ras诱导的转录激活，IC50为 10 nM。XRP44X 通过 FGF-2 抑制 Ras-Erk-1/2 通路激活。。XRP44X 是Elk3抑制剂；XRP44X 还对微管有影响。
| 生物活性 | XRP44X inhibitsRas-induced transcription activation with theIC50of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2[1]. XRP44X is an inhibitor of Ras/Erk activation ofElk3that also affectsmicrotubules[2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | XRP44X is an indirect inhibitor of Net phosphorylation that acts upstream from Erk-1/2 activation. XRP44X inhibits luciferase activity with the IC50of~10 nM[1].
XRP44X (10 nM) inhibits cell growth of HUVEC, NIH3T3, HCT-116, and NIH3T3–Ki-Ras cells[1].
XRP44X (100 nM) inhibits phosphorylation of Mek-1/2 and Raf-1[1].
Cell Proliferation Assay[1] | Cell Line: | HUVEC, NIH3T3, HCT-116, and NIH3T3-Ki-Ras cells | | Concentration: | 10 nM | | Incubation Time: | 24, 48, 72, 96 hours | | Result: | Inhibited HUVEC, HCT 116,NIH3T3, and NIH3T3-RAS cells proliferation with IC50s of 2.2±0.5 nM, 2.3±0.5 nM, 4±0.5 nM, and 2.3±0.5 nM, respectively.
Inhibited the growth of immortalized mouse fibroblasts. |
Western Blot Analysis[1] | Cell Line: | HUVEC cells | | Concentration: | 100 nM | | Incubation Time: | Pretreated for 90 minutes | | Result: | Inhibited phosphorylation of Rsk-1.
Inhibited phosphorylation of Erk-1/2 on sites required for its activation without affecting overall levels of Erk-1/2. |
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体内研究
(In Vivo) | XRP44X may have therapeutic potential for refractory asthma[1].
XRP44X, an inhibitor of Ras/Erk activation of the transcription factor Elk3, inhibits tumor growth and metastasis in mice. XRP44X inhibits tumor growth and metastasis in nude mice. XRP44X decreases the growth of tumours and the formation of metastases in nude mice[2].
| Animal Model: | Male nude mice (BALB/c nu/nu)[2] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; treated daily for 6 days | | Result: | Inhibited cell tumor formation by xenografts in nude mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(131.28 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6256 mL | 13.1278 mL | 26.2557 mL | | 5 mM | 0.5251 mL | 2.6256 mL | 5.2511 mL | | 10 mM | 0.2626 mL | 1.3128 mL | 2.6256 mL |
*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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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