CPL304110|cas:1627826-19-0|西域试剂

CPL304110,99.68%

产品编号：Bellancom-131908| CAS NO：1627826-19-0| 分子式：C₂₅H₃₀N₆O₂| 分子量：446.54

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货号	价格	库存与货期
Bellancom-131908	￥2200.00	杭州北京（现货）
Bellancom-131908	￥3500.00	杭州北京（现货）
Bellancom-131908	￥12300.00	杭州北京（现货）

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CPL304110

产品介绍

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 IC₅₀ values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	SNU-16 cell lines.
Concentration:	0-0.6 μM.
Incubation Time:	1 h.
Result:	Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human).
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%).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human).
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%).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human).
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%).

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (223.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。