SRX3207 是具有口服活性的、首创的Syk/PI3K双抑制剂,其对 Syk 和 PI3Kα 的IC50值分别为 10.7 nM 和 861 nM。SRX3207 缓解抗肿瘤免疫抑制。
生物活性 | SRX3207 is an orally active and first-in-class dualSyk/PI3Kinhibitor, withIC50values of 10.7 nM and 861 nM forSykandPI3Kα, respectively. SRX3207 relieves tumor immunosuppression[1][2]. |
IC50& Target[2] | Syk 10.7 nM (IC50) | PI3Kα 861 nM (IC50) | PI3Kδ 1280 nM (IC50) | PI3Kγ 11100 nM (IC50) | Zap70 1300 nM (IC50) |
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体外研究 (In Vitro) | SRX3207 (10 μmol/L) is able to block p-AKT at concentration[1]. SRX3207 has sufficient solubility in water (43 μmol/L)[1].
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体内研究 (In Vivo) | SRX3207 (10 mg/kg, orally) increases antitumor immune response[1].
Animal Model: | LLC or B16 or B16-OVA or CT26 (1 × 105) cells were injected subcutaneously into syngeneic mice[1]. | Dosage: | 10 mg/kg. | Administration: | Orally, starting from day 10 when tumors reached 100 mm3 until tumors were harvested on day 21. | Result: | Blocked phosphorylation of Syk at 348 site and Y525/526 site. Blocked immunosuppressive MΦ polarization. Blocked tumor growth and increased survival effectively.
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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 : 5 mg/mL(9.00 mM;Need ultrasonic) 配制储备液 1 mM | 1.7997 mL | 8.9985 mL | 17.9969 mL | 5 mM | 0.3599 mL | 1.7997 mL | 3.5994 mL | 10 mM | --- | --- | --- |
*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。 |