1. Protein Tyrosine Kinase/RTK
  2. FGFR c-Fms
  3. PRN1371

PRN1371 是高度选择性和有效的 FGFR1-4CSF1R 抑制剂,对FGFR1,FGFR2,FGFR3,FGFR4 和 CSF1R 的 IC50 值分别为 0.6,1.3,4.1,19.3 和 8.1 nM。

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PRN1371 Chemical Structure

PRN1371 Chemical Structure

CAS No. : 1802929-43-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2720
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1 mg ¥1000
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5 mg ¥2200
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10 mg ¥3900
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25 mg ¥7400
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MCE 顾客使用本产品发表的 1 篇科研文献

查看 FGFR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively[1].

IC50 & Target

FGFR1

0.6 nM (IC50)

FGFR2

1.3 nM (IC50)

FGFR3

4.1 nM (IC50)

FGFR4

19.3 nM (IC50)

CSF1R

8.1 nM (IC50)

体外研究
(In Vitro)

PRN1371 presents a unique profile of high biochemical and cellular potency (FGFR1 IC50=0.6 nM, SNU16 IC50=2.6 nM), prolonged target engagement (FGFR1 occupancy 24 h=96%), < 30% hERG inhibition at 1 μM, and good predicted ADME stability with BME reactivity Kd>100 μM. Broader kinome-wide biochemical profiling of PRN1371 against 251 kinases identifies only FGFR1−4 and CSF1R as being potently inhibited[1].

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

体内研究
(In Vivo)

PK studies of PRN1371 in rat, dog, and cynomolgus monkey show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing po (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirms the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant body weight loss. PRN1371 free base has been administered orally once daily as powder in a capsule on a 28-day continuous schedule. Human plasma concentrations for doses ranging from 15 to 35 mg confirm good oral exposure, rapid systemic clearance, no accumulation from day 1 to day 15, and a dose-dependent increase in AUC. Serum phosphate, a pharmacodynamic marker of FGFR inhibition, is increased for all doses studied and shows a dose-dependent increase between 20 and 35 mg, despite the administration of prophylactic phosphate binders[1].

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

Clinical Trial
分子量

561.46

Formula

C26H30Cl2N6O4

CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 25 mg/mL (44.53 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7811 mL 8.9054 mL 17.8107 mL
5 mM 0.3562 mL 1.7811 mL 3.5621 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.45 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.45 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

Enzyme inhibition is determined using a Caliper capillary electrophoresis system that separates phosphorylated and nonphosphorylated peptides on the basis of charge. Different concentrations of PRN1371 are first preincubated with enzyme for 15 min. The reaction is initiated with addition of peptide substrate, ATP, and Mg2+ and incubated at 25°C for 3 h. To stop the reaction, the mixture is quenched with EDTA. The buffer is 100 mM HEPES, pH 7.5, 0.1% BSA, 0.01% Triton X-100, 1 mM DTT, 10 mM MgCl2, 10 mM sodium orthovanadate, 10 μM β-glycerophosphate, and 1% DMSO. The ATP concentration of the reaction is at the predetermined value of the Km for ATP[1].

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

Cell Assay
[1]

SNU16 cells are first seeded into 384- well plates and PRN1371 added such that the highest final compound concentration is 5 μM. Cells are incubated with PRN1371 for 72 h at 37°C. To detect viability, the Presto-Blue cell viability reagent is added. Plates are read using an Analyst HT with a fluorescent mode employing 530 nm excitation and 590 nm emission[1].

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

Animal Administration
[1]

Mice: PRN1371 is evaluated in pharmacodynamics and efficacy studies using a SNU16 gastric cancer xenograft mouse model with high overexpression of FGFR2. In nude mice implanted with subcutaneous SNU16 tumors, pFGFR2 levels in the tumor are measured via Western blotting at 8 h following a 10 mg/kg oral dose. Low levels of pFGFR2 confirmed the ability of compound 34 to block FGFR2 activity in tumor tissue. Efficacy is determined by measuring tumor growth inhibition in the same SNU16 xenograft model[1].

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

参考文献

PRN1371 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7811 mL 8.9054 mL 17.8107 mL 44.5268 mL
5 mM 0.3562 mL 1.7811 mL 3.5621 mL 8.9054 mL
10 mM 0.1781 mL 0.8905 mL 1.7811 mL 4.4527 mL
15 mM 0.1187 mL 0.5937 mL 1.1874 mL 2.9685 mL
20 mM 0.0891 mL 0.4453 mL 0.8905 mL 2.2263 mL
25 mM 0.0712 mL 0.3562 mL 0.7124 mL 1.7811 mL
30 mM 0.0594 mL 0.2968 mL 0.5937 mL 1.4842 mL
40 mM 0.0445 mL 0.2226 mL 0.4453 mL 1.1132 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
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目录号:
HY-101768
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