2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. PF-4989216

PF-4989216 是一种有效的选择性 PI3Kα 抑制剂，Ki 为 0.6 nM。

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PF-4989216 Chemical Structure

PF-4989216 Chemical Structure

CAS No. : 1276553-09-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥880
In-stock
5 mg ￥800
In-stock
10 mg ￥1280
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50 mg ￥3900
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500 mg   询价  

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Customer Review

PF-4989216 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.

IC50 & Target[1]

PI3Kα

0.6 nM (Ki)

mTOR

1440 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
3.58 μM
Compound: 3; PF-4989216
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
[PMID: 32375077]
NCI-H1975 IC50
0.94 μM
Compound: 3; PF-4989216
Antiproliferative activity against human NCI-H1975 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
Antiproliferative activity against human NCI-H1975 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
[PMID: 32375077]
NCI-H460 IC50
0.12 μM
Compound: 3; PF-4989216
Antiproliferative activity against human NCI-H460 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
Antiproliferative activity against human NCI-H460 cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
[PMID: 32375077]
T47D IC50
0.34 μM
Compound: 3; PF-4989216
Antiproliferative activity against human T47D cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
Antiproliferative activity against human T47D cells harboring PIK3CA mutation assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
[PMID: 32375077]
U-87MG ATCC IC50
2.31 μM
Compound: 3; PF-4989216
Antiproliferative activity against human U87MG cells harboring PTEN deletion assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
Antiproliferative activity against human U87MG cells harboring PTEN deletion assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescence assay
[PMID: 32375077]
体外研究
(In Vitro)

PF-4989216 (Compound 10) has excellent PI3Kα Ki (0.6 nM), good cellular potency (S473 IC50=79 nM), and good selectivity against mTOR (mTOR Ki=1440 nM). PF-4989216 has PI3Kα Ki less than 1 nM and mTOR Ki more than 1 μM. PF-4989216 also has excellent selectivity over 40 other kinases, and no major CYP inhibitions are observed. Less than 30% inhibition is observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM[1]. The toxicity of PF-4989216 in several drug-sensitive and MDR cancer cell lines, including cells overexpressing ABCB1 or ABCG2, and in HEK293 cells transfected with human ABCB1 or ABCG2 is determined. PF-4989216 inhibits human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 with IC50s of 1.11±0.09 and 6.79±1.00 uM, respectively. PF-4989216 inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 IC50s of 2.30±0.68, 23.26±2.94 and 62.57±5.46 uM, respectively. PF-4989216 inhibits pcDNA-HEK293, ABCB1-transected MDR19-HEK293, ABCG2-tranfected R482-HEK293 cells with IC50s of 0.44±0.05, 0.38±0.06 and 5.05±0.89 uM, respectively[2].

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

PF-4989216 相关抗体:
体内研究
(In Vivo)

PF-4989216 (Compound 10) is dosed orally in our in vivo antitumor model, PI3K driven NCI-H1975 xenograft tumors. PF-4989216 demonstrates dose responsive tumor growth inhibitory activity from 25 to 200 mg/kg in QD oral dosing[1].

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

380.40

Formula

C18H13FN6OS
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
细胞实验： 

DMSO 中的溶解度 : ≥ 29 mg/mL (76.24 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6288 mL 13.1441 mL 26.2881 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 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

动物实验：

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 (6.57 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。

    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；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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.57 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，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

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

只
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
Cell Assay
[2]

MTT and CCK-8 assays are performed to determine the general sensitivities of cells to the tested drugs. The human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 are treated with PF-4989216 (0.1, 1 and 10 μM). The human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 are treated with PF-4989216 (0.1, 1, 10 and 100 μM).The parental HEK293 and ABCG2-tranfected R482-HEK293 cells are treated with PF-4989216 (0.01, 0.1, 1 and 10 μM). For the reversal of cytotoxicity assays, PF-4989216 or Ko143 or Lapatinib at a nontoxic concentration is added into the cytotoxicity assay, and the extent of reversal is then calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
For animal studies, 6-8 week old nu/nu athymic female mice are used. Tumors are established by injecting 2×106 cells suspended 1:1 (v/v) with reconstituted basement membrane. For tumor growth inhibition studies, mice with established tumors of ~150 mm3 are randomized. PF-4989216 (Compound 10) is dosed orally (25, 50, 100 and 200 mg/kg) in a mouse PI3K driven NCI-H1975 xenograft tumor model. Tumor dimensions are measured with vernier calipers, and tumor volumes are calculated. Tumor growth inhibition percentage (TGI %) is calculated.

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

PF-4989216 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 2.6288 mL 13.1441 mL 26.2881 mL 65.7203 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL 13.1441 mL
10 mM 0.2629 mL 1.3144 mL 2.6288 mL 6.5720 mL
15 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
20 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2860 mL
25 mM 0.1052 mL 0.5258 mL 1.0515 mL 2.6288 mL
30 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
40 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6430 mL
50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3144 mL
60 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 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.

Keywords:

PF-49892161276553-09-3PF4989216PF 4989216PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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