CPL304110|1627826-19-0|-陌孚医药/Medlife

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CPL304110

目录号: PL03248 纯度: ≥99%

CAS No. :1627826-19-0

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中文名称	CPL304110
英文名称	CPL304110
英文别名	CPL304110
Cas No.	1627826-19-0
分子式	C₂₅H₃₀N₆O₂
分子量	446.54
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情

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 of fibroblast growth factor receptors FGFR (1-3), with IC 50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

性状

Solid

IC50 & Target[1][2]

FGFR1 0.75 nM (IC50) FGFR2 0.5 nM (IC

体外研究(In Vitro)

CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK).
CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC50 of 85.64 nM.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

CPL304110 (p.o., 40 mg/kg) exhibits a t 1/2 of 2 h and C max of 3369 ng/mL in mice.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Abdellah Yamani, et al. Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). Eur J Med Chem. 2020 Nov 7;112990.

溶解度数据	In Vitro: DMSO : 100 mg/mL (223.94 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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