1. PI3K/Akt/mTOR Apoptosis
  2. PI3K Apoptosis
  3. PI3Kα-IN-9

PI3Kα-IN-9 (compound 27) 是一种有选择性的口服长效 PI3Kα 抑制剂 (PI3Kα inhibitor),对于 PI3Kα、PI3Kγ、PI3Kδ 和 PI3Kβ,其 IC50 值分别为 4.4、128、146 和 153 nM。PI3Kα-IN-9 具有抗增殖活性并诱导细胞凋亡。PI3Kα-IN-9 可用于癌症研究。

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PI3Kα-IN-9 Chemical Structure

PI3Kα-IN-9 Chemical Structure

CAS No. : 2715287-67-3

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research[1].

IC50 & Target[1]

PI3Kα

4.4 nM (IC50)

PI3Kβ

153 nM (IC50)

PI3Kδ

146 nM (IC50)

PI3Kγ

128 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
K562 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
MCF7 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
MDA-MB-231 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
MGC-803 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
MOLT-4 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
PC-3 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
RPMI-8226 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
SK-OV-3 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
U-251 IC50
0.43 μM
Compound: 27
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
[PMID: 35834807]
体外研究
(In Vitro)

PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis[1].
PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K[1].

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

Cell Viability Assay[1]

Cell Line: MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines
Concentration: 0-2 μM
Incubation Time: 72 hours
Result: Inhibited the growth of a variety of cancer cells with IC50 values ranging from 0.43 to 1.33 μM.

Apoptosis Analysis[1]

Cell Line: MGC-803 cells
Concentration: 0, 2, 4 and 8 μM
Incubation Time: 36 hours
Result: Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.
体内研究
(In Vivo)

PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T1/2>10 h) and high bioavailability (130%)[1].
PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity[1].

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

Animal Model: Male Sprague-Dawley rat[1]
Dosage: 1 and 10 mg/kg
Administration: Oral administration and intravenous injection; for 24 hours (Pharmacokinetic Analysis)
Result: 1.19
parameters IV PO
dose (mg/kg) 1 10
T1/2 (h) 6.29 ﹥10
Tmax (h) 0.003 9.33
Cmax (ng/mL) 454.7 2256.7
AUC0-t (ng·h/mL) 2237 36697
AUC0-∞ (ng·h/mL) 2922.4 38114.3
CL (mL/h/kg) 343
F % 130.4
Animal Model: Male BALB/c nude mice[1]
Dosage: 30 mg/kg
Administration: Oral administration; daily, for 3 weeks
Result: Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.
分子量

383.40

Formula

C18H21N7O3

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (260.82 mM; 超声助溶 (<80°C); 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 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 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, 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。

  • 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 (6.52 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL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 (6.52 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    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

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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6082 mL 13.0412 mL 26.0824 mL 65.2061 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL 13.0412 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL 6.5206 mL
15 mM 0.1739 mL 0.8694 mL 1.7388 mL 4.3471 mL
20 mM 0.1304 mL 0.6521 mL 1.3041 mL 3.2603 mL
25 mM 0.1043 mL 0.5216 mL 1.0433 mL 2.6082 mL
30 mM 0.0869 mL 0.4347 mL 0.8694 mL 2.1735 mL
40 mM 0.0652 mL 0.3260 mL 0.6521 mL 1.6302 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3041 mL
60 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8151 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6521 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:
PI3Kα-IN-9
目录号:
HY-150618
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