PF 477736 (Synonyms:PF 00477736)
目录号 : KM4750 CAS No. : 952021-60-2 纯度 : 98%

PF 477736 (PF 00477736) 是一种有效,选择性和 ATP 竞争性的 Chk1 的抑制剂,Ki 值为 0.49 nM。它也是 Chk2 抑制剂,Ki 值为 47 nM。PF 477736 显示出对 VEGFR2,Fms,Yes,Aurora-A,FGFR3,Flt3 和 Ret (IC50=8 (Ki),10,14,23,23,25 和 39 nM) <100 倍的选择性。PF 477736 在体外和体内均可增强 Gemcitabine 的抗肿瘤活性。

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200mg 询价 In-stock

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生物活性

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

体外研究

PF 477736 is a poor inhibitor of CDK1 activity (Ki=9.9 μM, 20,000-fold versus Chk1).
PF 477736 (0.01-1 μM; 16 h) dose-dependently abrogates the camptothecin-induced DNA damage checkpoint in CA46 cells.
PF 477736 (10-48 h) abrogates the Gemcitabine-induced S-phase arrest and induces increase in apoptotic cell death in HT29 cells.
PF 477736 (180-540 nM; 4-48 h) enhances Gemcitabine cytotoxicity in dose- and time-dependent manner in HT29 cells.

体内研究

PF 477736 (4-60 mg/kg; i.p. for once a day or twice a day for four treatments) potentiates Gemcitabine antitumor activity in Colo205 xenografts.
PF 477736 (15 and 30 mg/kg; i.p.) induces histone H3 phosphorylation and DNA damage and increases apoptosis in vivo.
PF 477736 (4 mg/kg; i.v.) exhibits low systemic plasma clearance (11.8 mL/min/kg) and terminal half-life (2.9 h) in rats.
PF 477736 (4-40 mg/kg; i.p.) exhibits a dose dependent pharmacokinetics.

分子式
C22H25N7O2
分子量
419.48
CAS号
952021-60-2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (297.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3839 mL 11.9195 mL 23.8390 mL
5 mM 0.4768 mL 2.3839 mL 4.7678 mL
10 mM 0.2384 mL 1.1920 mL 2.3839 mL
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: ≥ 2.08 mg/mL (4.96 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.96 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.96 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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