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iMDK {[allProObj[0].p_purity_real_show]}

货号:A1209466

iMDK是一种 PI3K 抑制剂,能够抑制生长因子 MDK(中期因子/MK),在联合 MEK 抑制剂时能协同抑制非小细胞肺癌 (NSCLC),同时对正常细胞和小鼠无明显毒性,具有癌症研究中的应用潜力。

iMDK 化学结构 CAS号:881970-80-5
iMDK 化学结构
CAS号:881970-80-5
iMDK 3D分子结构
CAS号:881970-80-5
iMDK 化学结构 CAS号:881970-80-5
iMDK 3D分子结构 CAS号:881970-80-5
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iMDK 纯度/质量文件 产品仅供科研

货号:A1209466 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 C2β p110α p110β p110γ p110δ PI3K Vps34 其他靶点 纯度
A66 +

C2β, IC50: 462 nM

++

p110α, IC50: 32 nM

99%+
Taselisib +

C2β, IC50: 292 nM

++++

PI3Kα, Ki: 0.29 nM

+++

PI3Kβ, Ki: 9.1 nM

++++

PI3Kγ, Ki: 0.97 nM

++++

PI3Kδ, Ki: 0.12 nM

+

hVps34, IC50: 374 nM

99%+
Gedatolisib ++++

PI3Kα, IC50: 0.4 nM

+++

PI3Kγ, IC50: 5.4 nM

mTOR 99%
HS-173 ++++

PI3Kα , IC50: 0.8 nM

99%+
Serabelisib +++

PI3Kα, IC50: 21 nM

99%+
GNE-477 ++++

PI3Kα, IC50: 4 nM

mTOR 99%
YM-201636 +

p110α, IC50: 3.3 μM

PIKfyve 98%
AS-252424 +

PI3Kα, IC50: 935 nM

++

PI3Kγ, IC50: 33 nM

99%
Alpelisib +++

PI3Kα, IC50: 5 nM

99%+
AS-604850 +

PI3Kα, IC50: 4.5 μM

+

PI3Kγ, IC50: 0.25 μM

99%
SF2523 ++

PI3Kα, IC50: 34 nM

++

PI3Kγ, IC50: 158 nM

DNA-PK,mTOR 99%+
Inavolisib ++++

PI3K alpha, IC50: 0.038 nM

99%+
Bimiralisib ++++

PI3Kα, Kd: 1.5 nM

+++

PI3Kβ, Kd: 11 nM

++

PI3Kγ, Kd: 25 nM

++

PI3Kδ, Kd: 25 nM

mTOR 99%+
GSK1059615 ++++

PI3Kα, IC50: 0.4 nM

++++

PI3Kβ, IC50: 0.6 nM

+++

PI3Kγ, IC50: 5 nM

++++

PI3Kδ, IC50: 2 nM

mTOR 98%
GSK2636771 99%
Fimepinostat +++

PI3Kα, IC50: 19 nM

++

PI3Kβ, IC50: 54 nM

++

PI3Kδ, IC50: 39 nM

99%+
VS-5584 ++++

PI3Kα, IC50: 2.6 nM

+++

PI3Kβ, IC50: 21 nM

++++

PI3Kγ, IC50: 3.0 nM

++++

PI3Kδ, IC50: 2.7 nM

mTOR 98%
Dactolisib ++++

p110α1, IC50: 4 nM

++

p110β, IC50: 75 nM

+++

p110γ, IC50: 5 nM

+++

p110δ, IC50: 7 nM

98+%
PI-103 ++++

p110α, IC50: 2 nM

++++

p110β, IC50: 3 nM

+++

p110γ, IC50: 15 nM

++++

p110δ, IC50: 3 nM

DNA-PK,mTOR 99%+
PI-3065 +

p110β, IC50: 1078 nM

+++

p110δ, IC50: 15 nM

99%+
Voxtalisib ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR 99%+
AZD-8835 +++

PI3Kα, IC50: 6.2 nM

+

PI3Kβ, IC50: 431 nM

++

PI3Kγ, IC50: 90 nM

+++

PI3Kδ, IC50: 5.7 nM

99%
Pilaralisib analogue ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 36 nM

+++

PI3Kγ, IC50: 23 nM

++

PI3Kδ, IC50: 36 nM

99%+
ZSTK474 +++

PI3Kα, IC50: 16 nM

++

PI3Kβ, IC50: 44 nM

++

PI3Kγ, IC50: 49 nM

+++

PI3Kδ, IC50: 4.6 nM

++

PI3K, IC50: 37 nM

98%
AS-605240 ++

PI3Kα, IC50: 60 nM

+

PI3Kβ, IC50: 270 nM

+++

PI3Kγ, IC50: 8 nM

+

PI3Kδ, IC50: 300 nM

98%
TGX-221 +++

p110β, IC50: 5 nM

++

p110δ, IC50: 0.1 μM

99%+
PF-04691502 ++++

PI3Kα, Ki: 1.8 nM

++++

PI3Kβ, Ki: 2.1 nM

++++

PI3Kγ, Ki: 1.9 nM

++++

PI3Kδ, Ki: 1.6 nM

mTOR 98+%
GDC-0084 ++++

PI3Kα, Ki app: 2 nM

++

PI3Kβ, Ki app: 46 nM

+++

PI3Kγ, Ki app: 10 nM

++++

PI3Kδ, Ki app: 3 nM

mTOR 99%+
Buparlisib ++

p110α, IC50: 52 nM

+

p110β, IC50: 166 nM

+

p110γ, IC50: 262 nM

++

p110δ, IC50: 116 nM

+

Vps34, IC50: 2.4 μM

mTOR 98%
LY294002 +

p110α, IC50: 0.5 μM

+

p110β, IC50: 0.97 μM

+

p110δ, IC50: 0.57 μM

DNA-PK 99%+
AZD 6482 +

PI3Kα, IC50: 870 nM

+++

PI3Kβ, IC50: 10 nM

++

PI3Kδ, IC50: 80 nM

DNA-PK 99%+
Pictilisib ++++

p110α, IC50: 3 nM

++

p110β, IC50: 33 nM

++

p110γ, IC50: 75 nM

++++

p110δ, IC50: 3 nM

mTOR 99%+
PKI-402 ++++

PI3Kα, IC50: 2 nM

+++

PI3Kβ, IC50: 7 nM

+++

PI3Kγ, IC50: 16 nM

+++

PI3Kδ, IC50: 14 nM

mTOR 98%
Copanlisib ++++

PI3Kα, IC50: 0.5 nM

++++

PI3Kβ, IC50: 3.7 nM

+++

PI3Kγ, IC50: 6.4 nM

++++

PI3Kδ, IC50: 0.7 nM

99%+
Omipalisib ++++

p110α, Ki: 0.019 nM

++++

p110β, Ki: 0.13 nM

++++

p110γ, Ki: 0.06 nM

++++

p110δ, Ki: 0.024 nM

99%+
Izorlisib +++

PI3Kα, IC50: 14 nM

++

PI3Kβ, IC50: 0.12 μM

++

PI3Kγ, IC50: 36 nM

+

PI3Kδ, IC50: 0.50 μM

99%+
AZD8186 ++

PI3Kα, IC50: 35 nM

++++

PI3Kβ, IC50: 4 nM

+++

PI3Kδ, IC50: 12 nM

99%
KU-0060648 ++++

PI3Kα, IC50: 4 nM

++++

PI3Kβ, IC50: 0.5 nM

+

PI3Kγ, IC50: 0.59 μM

++++

PI3Kδ, IC50: 0.1 nM

DNA-PK 98%
Apitolisib +++

p110α, IC50: 5 nM

++

p110β, IC50: 27 nM

+++

p110γ, IC50: 14 nM

+++

p110δ, IC50: 7 nM

mTOR 98%+
CZC24832 +

PI3Kβ, IC50: 1.1 μM

++

PI3Kγ, IC50: 27 nM

98+%
BGT226 maleate ++++

PI3Kα, IC50: 4 nM

++

PI3Kβ, IC50: 63 nM

++

PI3Kγ, IC50: 38 nM

mTOR 99%+
TG 100713 ++

PI3Kα, IC50: 165 nM

+

PI3Kβ, IC50: 215 nM

++

PI3Kγ, IC50: 50 nM

+++

PI3Kδ, IC50: 24 nM

98%+
PI3K-IN-1 ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR 98+%
TG100-115 +

PI3Kα, IC50: 1.3 μM

+

PI3Kβ, IC50: 1.2 μM

++

PI3Kγ, IC50: 83 nM

+

PI3Kδ, IC50: 235 nM

98%
PIK-90 +++

PI3Kα, IC50: 11 nM

+

PI3Kβ, IC50: 350 nM

+++

PI3Kγ, IC50: 18 nM

++

PI3Kδ, IC50: 58 nM

99%+
PIK-294 +

p110β, IC50: 490 nM

++

p110γ, IC50: 160 nM

+++

p110δ, IC50: 10 nM

99%+
Duvelisib ++++

PI3Kβ, Ki: 1564 pM

++

PI3Kγ, Ki: 243 pM

++++

PI3Kδ, Ki: 23 pM

99%+
GDC-0326 ++++

PI3Kα, Ki: 0.2 nM

++

PI3Kβ, Ki: 26.6 nM

+++

PI3Kγ, Ki: 10.2 nM

++++

PI3Kδ, Ki: 4 nM

98%
Quercetin Dihydrate +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

95%
Quercetin +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

PKC,Sirtuin,Src 95%
Leniolisib +

PI3Kα, IC50: 0.244 μM

+

PI3Kβ, IC50: 0.424 μM

+

PI3Kγ, IC50: 2.23 μM

+++

PI3Kδ, IC50: 0.011 μM

DNA-PK 99%+
PIK-108 99%
Eganelisib +++

PI3Kγ, IC50: 16 nM

99%+
CAY10505 99%
IPI-3063 ++++

p110δ, IC50: 2.5 nM

99%
Nemiralisib ++++

PI3Kδ, pKi: 9.9

99%+
PF-4989216 ++++

p110α, IC50: 2 nM

++

p110γ, IC50: 65 nM

++++

p110δ, IC50: 1 nM

99%+
PIK-75 HCl +++

p110α, IC50: 5.8 nM

++

p110γ, IC50: 76 nM

+

p110δ, IC50: 0.51 μM

DNA-PK 99%+
Tenalisib ++

PI3Kγ, IC50: 33.2 nM

++

PI3Kδ, IC50: 24.5 nM

98%
Acalisib +++

p110δ, IC50: 14 nM

99%+
Umbralisib +++

PI3Kδ, IC50: 22.2 nM

99%+
AMG319 +

PI3Kγ, IC50: 850 nM

+++

PI3Kδ, IC50: 18 nM

99%
IC-87114 +

PI3Kγ, IC50: 29 μM

+

PI3Kδ, IC50: 0.5 μM

99%+
Idelalisib ++

p110γ, IC50: 89 nM

++++

p110δ, IC50: 2.5 nM

98%
PIK-293 +

p110γ, IC50: 10 μM

+

p110δ, IC50: 0.24 μM

99%+
Vps34-PIK-III +

PI3Kδ, IC50: 1.2μM

+++

Vps34, IC50: 0.018μM

99%+
GSK2292767 98%
Seletalisib +

PI3Kγ, IC50: 282 nM

+++

PI3Kδ, IC50: 12 nM

99%+
P110δ-IN-1 ++++

P110δ, IC50: 0.6 nM

99%
PI3Kδ-IN-5 ++++

PI3Kδ, IC50: 0.9 nM

99%
SRX3207 +

PI3K alpha, IC50: 244 nM

+

PI3K gamma, IC50: 9790 nM

+

PI3K delta, IC50: 388 nM

Syk 98%
Parsaclisib HCl ++++

PI3Kδ, IC50: 1 nM

98%
IHMT-PI3Kδ-372 +++

PI3Kδ, IC50: 14 nM

98%
Trigonelline Akt 99%+
Wortmannin ++++

PI3K, IC50: 3 nM

MLCK,DNA-PK 99%+
Samotolisib DNA-PK 99%+
GNE-317 99%+
Oroxin B Akt,PTEN 99%+
NU 7026 +

PI3K, IC50: 13 μM

DNA-PK 98+%
Deguelin Akt 99%+
Ailanthone ATM/ATR,Akt,CDK 98%
Resibufogenin ROS 98%
KU-57788 +

PI3K, IC50: 5 μM

DNA-PK,mTOR 99%+
Cinobufagine Akt 99%
α-Linolenic acid 97% (GC)
MTX-211 EGFR 98%
PI3K/mTOR Inhibitor-2 ++++

PI3K, IC50: 3.4 nM

mTOR 99%+
SPP-86 99%+
(E)-Akt inhibitor-IV 98%
Vps34-IN-1 ++

Vps34, IC50: 25 nM

98%
SAR405 ++++

Vps34, IC50: 1.2 nM

98+%
3-Methyladenine +

PI3Kγ, IC50: 60 μM

+

Vps34, IC50: 25 μM

Autophagy 98%
Vps34-IN-4 +++

VPS34, IC50: 15 nM

98%+
Autophinib +++

Vps34, IC50: 19 nM

Autophagy 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

iMDK 细胞实验

Cell Line
Concentration Treated Time Description References
MeT-5A 7.5, 15, 50 µM 72 hours To evaluate the effect of iMDK on the proliferation of MeT-5A cells, results showed significant inhibition of cell proliferation at the highest dose (50 µM). Cancer Gene Ther. 2024 Nov;31(11):1708-1720
MSTO-211H 7.5, 15, 50 µM 72 hours To evaluate the effect of iMDK on the proliferation of MSTO-211H cells, results showed significant inhibition of cell proliferation at the highest dose (50 µM). Cancer Gene Ther. 2024 Nov;31(11):1708-1720
colon cancer cell line HCT116 100nM 48 hours Inhibited MDK expression, reversed IFN-γ-activated EMT and tumor metastasis Front Oncol. 2022 Jun 7;12:885656
breast cancer cell line BT549 100nM 48 hours Inhibited MDK expression, reversed IFN-γ-activated EMT and tumor metastasis Front Oncol. 2022 Jun 7;12:885656
cervical carcinoma cell line CaSki 100nM 48 hours Inhibited MDK expression, reversed IFN-γ-activated EMT and tumor metastasis Front Oncol. 2022 Jun 7;12:885656
lung cancer cell line A549 100nM 48 hours Inhibited MDK expression, reversed IFN-γ-activated EMT and tumor metastasis Front Oncol. 2022 Jun 7;12:885656
kidney cancer cell line Caki-1 100nM 48 hours Inhibited MDK expression, reversed IFN-γ-activated EMT and tumor metastasis Front Oncol. 2022 Jun 7;12:885656
HUVEC cells 10 μM 5 hours To evaluate the effect of iMDK on HUVEC tube formation, results showed that iMDK combined with PD0325901 significantly inhibited tube formation Exp Cell Res. 2015 Jul 15;335(2):197-206
A549 cells 0.25 μM 72 hours To evaluate the inhibitory effect of iMDK on A549 cell proliferation, results showed that iMDK alone did not inhibit cell proliferation, but significantly inhibited cell proliferation when combined with PD0325901 Exp Cell Res. 2015 Jul 15;335(2):197-206
H520 cells 0.125 μM 72 hours To evaluate the inhibitory effect of iMDK on H520 cell proliferation, results showed that iMDK significantly inhibited cell proliferation Exp Cell Res. 2015 Jul 15;335(2):197-206
H2009 cells 1 μM 24 hours To evaluate the effect of iMDK on H2009 cell colony formation, results showed that iMDK significantly reduced colony formation Exp Cell Res. 2015 Jul 15;335(2):197-206
H441 cells 2.5 μM 72 hours To evaluate the inhibitory effect of iMDK on H441 cell proliferation, results showed that iMDK significantly inhibited cell proliferation Exp Cell Res. 2015 Jul 15;335(2):197-206
SKOV3 human ovarian cancer cell line 100 nM To assess the effect of iMDK on IFN-γ-induced EMT and metastasis, found that iMDK significantly suppressed IFN-γ-driven EMT and metastasis Biomedicines. 2022 Dec 21;11(1):8
SKOV3 human ovarian cancer cell line 6.6 nM 48 hours To assess the effect of iMDK on IFN-γ-induced anti-proliferation, found that iMDK significantly enhanced the anti-tumor activity of IFN-γ Biomedicines. 2022 Dec 21;11(1):8
NHLF normal human lung fibroblast cells 5-500 nM 48 hours iMDK had no significant effect on NHLF cells PLoS One. 2013 Aug 16;8(8):e71093
A549 lung adenocarcinoma cells 5-500 nM 48 hours iMDK had no significant effect on A549 cells PLoS One. 2013 Aug 16;8(8):e71093
H520 human lung squamous cell carcinoma cells 5-500 nM 48 hours iMDK inhibited H520 cell growth PLoS One. 2013 Aug 16;8(8):e71093
H441 lung adenocarcinoma cells 5-500 nM 48 hours iMDK inhibited H441 cell growth by suppressing the PI3K pathway and inducing apoptosis PLoS One. 2013 Aug 16;8(8):e71093
Caco-2 cells 25 nM 72 hours To investigate the effect of iMDK on the permeability of tight junctions in MPA-treated Caco-2 cell monolayers. Results showed that iMDK significantly inhibited MPA-induced compromised TJ integrity. Front Physiol. 2017 Jun 26;8:438
neural progenitors (NP) 0.5 μM 5 days Evaluate the effect of idebenone on NP cell viability, showing no significant change at 0.5 μM concentration. Biogerontology. 2017 Aug;18(4):665-677
early neural progenitors (eNP) 0.5 μM 5 days Evaluate the effect of idebenone on eNP cell viability, showing a significant increase to 138.19% at 0.5 μM concentration. Biogerontology. 2017 Aug;18(4):665-677
neural stem cells (NSC) 0.5 μM 5 days Evaluate the effect of idebenone on NSC cell viability, showing a significant increase to 130% at 0.5 μM concentration. Biogerontology. 2017 Aug;18(4):665-677

iMDK 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft model Intraperitoneal injection 9 mg/kg Once every two days IMDK significantly reduced tumor volume and weight and decreased lung metastasis rates Cancers (Basel). 2020 Aug 24;12(9):2402
BALB/c nude mice H441 cell xenograft model IMDK: intraperitoneal injection, PD0325901: oral administration iMDK: 9 mg/kg, PD0325901: 5 mg/kg IMDK: once daily, PD0325901: five times per week, for 11 days To evaluate the inhibitory effect of iMDK combined with PD0325901 on H441 cell xenograft tumor growth, results showed that the combination therapy significantly inhibited tumor growth and tumor-associated angiogenesis Exp Cell Res. 2015 Jul 15;335(2):197-206
BALB/c nude mice H441 lung adenocarcinoma xenograft model Intraperitoneal injection 9 mg/kg 3 or 5 times per week for 10 days IMDK significantly inhibited tumor growth by suppressing the PI3K pathway and inducing apoptosis PLoS One. 2013 Aug 16;8(8):e71093

iMDK 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.28mL

2.66mL

1.33mL

26.57mL

5.31mL

2.66mL

iMDK 技术信息

CAS号881970-80-5
分子式C21H13FN2O2S
分子量 376.4
SMILES Code O=C1C(C2=CN3C(SC(CC4=CC=C(F)C=C4)=C3)=N2)=CC5=C(O1)C=CC=C5
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 3 mg/mL(7.97 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
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