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PF-3758309 (Synonyms: PF-03758309) 纯度: 98.52%
PF-3758309 (PF-03758309) 是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (Kd= 2.7 nM; Ki=18.7 nM)。PF-3758309 具有 PAK4 抑制剂的预期细胞功能:抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。
PF-3758309 Chemical Structure
CAS No. : 898044-15-0
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥605 | In-stock | |
5 mg | ¥550 | In-stock | |
10 mg | ¥800 | In-stock | |
50 mg | ¥2600 | In-stock | |
100 mg | ¥4400 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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PF-3758309 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Cell Cycle/DNA Damage Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Cytoskeleton Compound Library
- Orally Active Compound Library
- Chemical Probe Library
- Targeted Diversity Library
生物活性 |
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM)[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) |
PF-3758309 (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models[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 |
490.62 |
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Formula |
C25H30N8OS |
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CAS 号 |
898044-15-0 |
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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 : ≥ 100 mg/mL (203.82 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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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