CPL304110 是有效的、口服有效的、选择性的成纤维细胞生长因子受体FGFR (1-3)的抑制剂,其对 FGFR (1-3) 的IC50值分别为 0.75 nM、0.5 nM 和 3.05 nM。
生物活性 | CPL304110 is a potent, orally active and selective inhibitor offibroblast growth factorreceptorsFGFR(1-3), withIC50values of 0.75 nM, 0.5 nM, and 3.05 nM forFGFR(1-3), respectively[1]. |
IC50& Target[1] | FGFR1 0.75 nM (IC50) | FGFR2 0.5 nM (IC50) | FGFR3 3.05 nM (IC50) |
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体外研究 (In Vitro) | CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK)[1]. CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC50of 85.64 nM[1]. CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases[1].
Western Blot Analysis[1] Cell Line: | SNU-16 cell lines. | Concentration: | 0-0.6 μM. | Incubation Time: | 1 h. | Result: | Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK) |
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体内研究 (In Vivo) | CPL304110 (p.o., 40 mg/kg) exhibits a t1/2of 2 h and Cmaxof 3369 ng/mL in mice[1]. CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day[1].
Animal Model: | Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human)[1]. | Dosage: | 20 mg/kg (X2). | Administration: | Orally, twice daily for 21 days. | Result: | After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%). |
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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(223.94 mM;Need ultrasonic) 配制储备液 1 mM | 2.2394 mL | 11.1972 mL | 22.3944 mL | 5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 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。 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 分比是指该溶剂在您配制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 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.60 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.60 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.60 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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