PF-04691502 | PF4691502 | PI3K/mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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PF-04691502 {[allProObj[0].p_purity_real_show]}

货号：A300869 同义名： PF4691502

PF-04691502 is an ATP-competitive PI3K (α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.

PF-04691502 化学结构
CAS号：1013101-36-4

PF-04691502 3D分子结构
CAS号：1013101-36-4

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PF-04691502 纯度/质量文件产品仅供科研

货号：A300869 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

mTOR 亚型比较
PI3K 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (truncated), IC50: 0.13 nM mTOR (full length), IC50: 0.8 nM				{[allProObj[0].p_purity_real_show]}
Gedatolisib	++++ mTOR, IC50: 1.6 nM				{[allProObj[0].p_purity_real_show]}
GSK1059615	++ mTOR, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
Vistusertib	+++ mTOR, IC50: 2.8 nM				{[allProObj[0].p_purity_real_show]}
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	{[allProObj[0].p_purity_real_show]}
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				{[allProObj[0].p_purity_real_show]}
PI-103	+ mTOR, IC50: 30 nM				{[allProObj[0].p_purity_real_show]}
WAY-600	++ mTOR, IC50: 9 nM				{[allProObj[0].p_purity_real_show]}
Voxtalisib	+ mTOR, IC50: 157 nM				{[allProObj[0].p_purity_real_show]}
PF-04691502	++ mTOR, Ki: 16 nM				{[allProObj[0].p_purity_real_show]}
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Chrysophanol	✔			EGFR	{[allProObj[0].p_purity_real_show]}
Samotolisib	✔			DNA-PK	{[allProObj[0].p_purity_real_show]}
Torkinib	+++ mTOR, IC50: 8 nM			DNA-PK,PDGFR	{[allProObj[0].p_purity_real_show]}
Everolimus					{[allProObj[0].p_purity_real_show]}
WYE-354	+++ mTOR, IC50: 5 nM				{[allProObj[0].p_purity_real_show]}
Tacrolimus	✔				{[allProObj[0].p_purity_real_show]}
PP121	++ mTOR, IC50: 13 nM			VEGFR,PDGFR	{[allProObj[0].p_purity_real_show]}
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Rapamycin	++++ mTOR, IC50: ~0.1 nM				{[allProObj[0].p_purity_real_show]}
GDC-0349	+++ mTOR, Ki: 3.8 nM				{[allProObj[0].p_purity_real_show]}
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		{[allProObj[0].p_purity_real_show]}
WYE-687	+++ mTOR, IC50: 7 nM				{[allProObj[0].p_purity_real_show]}
Apitolisib	+ mTOR, Ki app: 17 nM				{[allProObj[0].p_purity_real_show]}
WYE-132	++++ mTOR, IC50: 0.19 nM				{[allProObj[0].p_purity_real_show]}
Sapanisertib	++++ mTOR, Ki: 1.4 nM				{[allProObj[0].p_purity_real_show]}
BGT226 maleate	✔				{[allProObj[0].p_purity_real_show]}
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
PI3K-IN-1	+ mTOR, IC50: 157 nM				{[allProObj[0].p_purity_real_show]}
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				{[allProObj[0].p_purity_real_show]}
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		{[allProObj[0].p_purity_real_show]}
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				{[allProObj[0].p_purity_real_show]}
Temsirolimus	+ mTOR, IC50: 1.76 μM				{[allProObj[0].p_purity_real_show]}
CZ415	++ mTOR, pIC50: 8.07				{[allProObj[0].p_purity_real_show]}
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		{[allProObj[0].p_purity_real_show]}
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		{[allProObj[0].p_purity_real_show]}
Palomid 529		✔			{[allProObj[0].p_purity_real_show]}
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。

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							{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	{[allProObj[0].p_purity_real_show]}
HS-173		++++ PI3Kα , IC50: 0.8 nM							{[allProObj[0].p_purity_real_show]}
Serabelisib		+++ PI3Kα, IC50: 21 nM							{[allProObj[0].p_purity_real_show]}
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	{[allProObj[0].p_purity_real_show]}
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	{[allProObj[0].p_purity_real_show]}
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					{[allProObj[0].p_purity_real_show]}
Alpelisib		+++ PI3Kα, IC50: 5 nM							{[allProObj[0].p_purity_real_show]}
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					{[allProObj[0].p_purity_real_show]}
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							{[allProObj[0].p_purity_real_show]}
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GSK2636771			✔						{[allProObj[0].p_purity_real_show]}
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				{[allProObj[0].p_purity_real_show]}
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				{[allProObj[0].p_purity_real_show]}
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				{[allProObj[0].p_purity_real_show]}
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				{[allProObj[0].p_purity_real_show]}
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				{[allProObj[0].p_purity_real_show]}
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			{[allProObj[0].p_purity_real_show]}
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				{[allProObj[0].p_purity_real_show]}
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				{[allProObj[0].p_purity_real_show]}
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	{[allProObj[0].p_purity_real_show]}
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	{[allProObj[0].p_purity_real_show]}
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				{[allProObj[0].p_purity_real_show]}
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				{[allProObj[0].p_purity_real_show]}
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				{[allProObj[0].p_purity_real_show]}
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	{[allProObj[0].p_purity_real_show]}
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					{[allProObj[0].p_purity_real_show]}
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	{[allProObj[0].p_purity_real_show]}
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				{[allProObj[0].p_purity_real_show]}
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				{[allProObj[0].p_purity_real_show]}
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				{[allProObj[0].p_purity_real_show]}
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				{[allProObj[0].p_purity_real_show]}
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				{[allProObj[0].p_purity_real_show]}
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				{[allProObj[0].p_purity_real_show]}
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				{[allProObj[0].p_purity_real_show]}
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	{[allProObj[0].p_purity_real_show]}
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
PIK-108			✔						{[allProObj[0].p_purity_real_show]}
Eganelisib				+++ PI3Kγ, IC50: 16 nM					{[allProObj[0].p_purity_real_show]}
CAY10505				✔					{[allProObj[0].p_purity_real_show]}
IPI-3063					++++ p110δ, IC50: 2.5 nM				{[allProObj[0].p_purity_real_show]}
Nemiralisib					++++ PI3Kδ, pKi: 9.9				{[allProObj[0].p_purity_real_show]}
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				{[allProObj[0].p_purity_real_show]}
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				{[allProObj[0].p_purity_real_show]}
Acalisib					+++ p110δ, IC50: 14 nM				{[allProObj[0].p_purity_real_show]}
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				{[allProObj[0].p_purity_real_show]}
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				{[allProObj[0].p_purity_real_show]}
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				{[allProObj[0].p_purity_real_show]}
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				{[allProObj[0].p_purity_real_show]}
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				{[allProObj[0].p_purity_real_show]}
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		{[allProObj[0].p_purity_real_show]}
GSK2292767					✔				{[allProObj[0].p_purity_real_show]}
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				{[allProObj[0].p_purity_real_show]}
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				{[allProObj[0].p_purity_real_show]}
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	{[allProObj[0].p_purity_real_show]}
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				{[allProObj[0].p_purity_real_show]}
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				{[allProObj[0].p_purity_real_show]}
Trigonelline						✔		Akt	{[allProObj[0].p_purity_real_show]}
Wortmannin						++++ PI3K, IC50: 3 nM		MLCK,DNA-PK	{[allProObj[0].p_purity_real_show]}
Samotolisib						✔		DNA-PK	{[allProObj[0].p_purity_real_show]}
GNE-317						✔			{[allProObj[0].p_purity_real_show]}
Oroxin B						✔		PTEN,Akt	{[allProObj[0].p_purity_real_show]}
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	{[allProObj[0].p_purity_real_show]}
Deguelin						✔		Akt	{[allProObj[0].p_purity_real_show]}
Ailanthone						✔		Akt,ATM/ATR,CDK	{[allProObj[0].p_purity_real_show]}
Resibufogenin						✔		ROS	{[allProObj[0].p_purity_real_show]}
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
Cinobufagine						✔		Akt	{[allProObj[0].p_purity_real_show]}
α-Linolenic acid						✔			{[allProObj[0].p_purity_real_show]}
MTX-211						✔		EGFR	{[allProObj[0].p_purity_real_show]}
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	{[allProObj[0].p_purity_real_show]}
SPP-86						✔			{[allProObj[0].p_purity_real_show]}
(E)-Akt inhibitor-IV						✔			{[allProObj[0].p_purity_real_show]}
Vps34-IN-1							++ Vps34, IC50: 25 nM		{[allProObj[0].p_purity_real_show]}
SAR405							++++ Vps34, IC50: 1.2 nM		{[allProObj[0].p_purity_real_show]}
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	{[allProObj[0].p_purity_real_show]}
Vps34-IN-4							+++ VPS34, IC50: 15 nM		{[allProObj[0].p_purity_real_show]}
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	{[allProObj[0].p_purity_real_show]}
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。

PF-04691502 生物活性

靶点

p110γ

PI3Kγ, Ki:1.9 nM
p110β

PI3Kβ, Ki:2.1 nM
p110α

PI3Kα, Ki:1.8 nM
p110δ

PI3Kδ, Ki:1.6 nM

描述

The phosphoinositide 3-kinase (PI3K) signaling pathway plays a central role in regulating cell growth, proliferation, survival, angiogenesis, metabolism, and motility. PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor, which potently inhibited recombinant class I PI3K and mTOR in biochemical assays and suppressed transformation of avian fibroblasts mediated by wild-type PI3K γ, δ, or mutant PI3Kα. Dual PI3K/mTOR inhibitors may most effectively block the PI3K pathway, overcome feedback loops, and block PI3K-independent mTOR activation. PF-04691502 inhibited human and mouse PI3Kα with Ki of 1.8 and 1.2 nmol/L, respectively, PI3K isoforms β, δ, and γ with Ki of 2.1, 1.6, and 1.9 nmol/L, respectively, and human mTOR with Ki of 16 nmol/L. PF-04691502 inhibited phosphorylation of AKT at S473 and T308 consistent with the inhibition of phosphorylation of AKT downstream proteins such as FKHRL1 and PRAS40. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 reduced phosphorylation of AKT T308 and AKT S473 (IC50 of 7.5 – 47 nmol/L and 3.8 – 20 nmol/L, respectively) and inhibited cell proliferation (IC50 of 179 – 313 nmol/L). PF-04691502 inhibited mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC50 of 32 nmol/L and inhibited the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. In a vivo study, PF-04691502 was formulated in 0.5% methylcellulose in water suspension, nude mice bearing U87MG tumors were administered orally once a day with PF-04691502 at 0.5, 1, 5, and 10 mg/kg. Dose-dependent tumor growth inhibition (TGI) was obtained in the U87MG xenograft model and approximately 73% TGI was observed at the MTD dose of 10 mg/kg^[3].

PF-04691502 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human BT20 cells		Function assay		Inhibition of AKT phosphorylation at Ser 473 in human BT20 cells, IC50=0.013 μM	23506825
human SKOV3 cells		Proliferation assay	3 days	Antiproliferative activity against human SKOV3 cells after 3 days by CellTiter-Glo assay, IC50=0.29 μM	25139570
human U87MG cells		Proliferation assay	4 days	Antiproliferative activity against human U87MG cells after 4 days by CellTiter-Glo assay, IC50=0.52 μM	25139570

PF-04691502 动物研究

Dose	Nude mice: 0.5 mg/kg - 10 mg/kg^[3] (p.o.); 10 mg/kg^[4] (i.v., q2w)
Administration	p.o.

PF-04691502 参考文献

[1]Simmons BH, Lee JH, et al. Combination of a MEK inhibitor at sub-MTD with a PI3K/mTOR inhibitor significantly suppresses growth of lung adenocarcinoma tumors in Kras(G12D-LSL) mice. Cancer Chemother Pharmacol. 2012 Aug;70(2):213-20.

[2]Kinross KM, Brown DV, et al. In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras(G12D);Pten deletion mouse model of ovarian cancer. Mol Cancer Ther. 2011 Aug;10(8):1440-9.

[3]Yuan J, Mehta PP, Yin MJ, Sun S, Zou A, Chen J, Rafidi K, Feng Z, Nickel J, Engebretsen J, Hallin J, Blasina A, Zhang E, Nguyen L, Sun M, Vogt PK, McHarg A, Cheng H, Christensen JG, Kan JL, Bagrodia S. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189-99. doi: 10.1158/1535-7163.MCT-11-0185. Epub 2011 Jul 12. PMID: 21750219.

PF-04691502 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.75mL

2.35mL

1.18mL

23.50mL

4.70mL

2.35mL

PF-04691502 技术信息

CAS号	1013101-36-4
分子式	C₂₂H₂₇N₅O₄
分子量	425.481

别名	PF4691502
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(117.51 mM)，配合低频超声助溶，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

动物实验配方

PF-04691502 {[allProObj[0].p_purity_real_show]}

PF-04691502 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PF-04691502 质控信息

PF-04691502 生物活性

PF-04691502 细胞研究

PF-04691502 动物研究

PF-04691502 参考文献

PF-04691502 实验方案

PF-04691502 技术信息

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p110γ	PI3Kγ, Ki:1.9 nM
p110β	PI3Kβ, Ki:2.1 nM
p110α	PI3Kα, Ki:1.8 nM
p110δ	PI3Kδ, Ki:1.6 nM
Akt	P-Akt (S473), IC50:3.8 nM P-Akt (T308), IC50:7.5 nM
mTOR	mTOR, Ki:16 nM

PF-04691502 {[allProObj[0].p_purity_real_show]}

PF-04691502 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PF-04691502 质控信息

PF-04691502 生物活性

PF-04691502 细胞研究

PF-04691502 动物研究

PF-04691502 参考文献

PF-04691502 实验方案

PF-04691502 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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PF-04691502 纯度/质量文件产品仅供科研