PF-4989216 | PI3K Inhibitor | AmBeed-信号通路专用抑制剂

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PF-4989216 {[allProObj[0].p_purity_real_show]}

货号：A607709

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

PF-4989216 化学结构
CAS号：1276553-09-3

PF-4989216 3D分子结构
CAS号：1276553-09-3

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PF-4989216 纯度/质量文件产品仅供科研

货号：A607709 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 >

PI3K 亚型比较
DUB 亚型比较

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。

产品名称	DUB ↓ ↑	UCH ↓ ↑	USP/UBP ↓ ↑	其他靶点	纯度
PR-619	+ Plpro, EC50: 14.2 μM	+++ UCH-L5, EC50: 12.8 μM UCH-L3, EC50: 2.95 μM	+++ USP5, EC50: 4.90 μM USP28, EC50: 6.24 μM		{[allProObj[0].p_purity_real_show]}
Degrasyn	✔			Bcr-Abl	{[allProObj[0].p_purity_real_show]}
VLX1570	+ DUB, IC50: ~10 μM				{[allProObj[0].p_purity_real_show]}
ML-323	++++ USP1-UAF1, IC50: 76 nM				{[allProObj[0].p_purity_real_show]}
LDN-57444		++++ UCH-L1, IC50: 0.4 μM UCH-L3, IC50: 25 μM			{[allProObj[0].p_purity_real_show]}
TCID		++++ UCH-L3, IC50: 0.6 μM			{[allProObj[0].p_purity_real_show]}
b-AP15		+++ UCHL5, IC50: 2.1 μM			{[allProObj[0].p_purity_real_show]}
P 22077			++ USP7, IC50: 8.6 μM USP47, EC50: 8.74 μM		{[allProObj[0].p_purity_real_show]}
P005091			++ USP7, EC50: 4.2 μM USP47, IC50: 4.3 μM		{[allProObj[0].p_purity_real_show]}
IU1			++ USP14, IC50: 4.7 μM		{[allProObj[0].p_purity_real_show]}
NSC632839			+ USP7, EC50: 37 μM USP2, EC50: 45 μM		{[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-4989216 生物活性

靶点	p110γ p110γ, IC50:65 nM p110α p110α, IC50:2 nM p110δ p110δ, IC50:1 nM
描述	PF-4989216 possesses outstanding PI3Kα Ki (0.6 nM), good cellular potency with S473 IC50 of 79 nM, and high selectivity against mTOR with mTOR Ki of 1440 nM. It exhibits excellent selectivity against over 40 other kinases, with minimal major CYP inhibitions. Inhibition levels of less than 30% are observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM ^[1]. The toxicity profile of PF-4989216 is evaluated across various drug-sensitive and multidrug-resistant (MDR) cancer cell lines, including those overexpressing ABCB1 or ABCG2, as well as in HEK293 cells transfected with human ABCB1 or ABCG2. PF-4989216 exhibits inhibitory effects on human colon carcinoma S1 cells and ABCG2-overexpressing subline S1-M1-80 with IC50 values of 1.11±0.09 and 6.79±1.00 μM, respectively. It also inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 with IC50 values of 2.30±0.68, 23.26±2.94, and 62.57±5.46 μM, respectively. Moreover, PF-4989216 inhibits pcDNA-HEK293, ABCB1-transfected MDR19-HEK293, and ABCG2-transfected R482-HEK293 cells with IC50 values of 0.44±0.05, 0.38±0.06, and 5.05±0.89 μM, respectively ^[2].
体内研究	PF-4989216, administered orally, demonstrates dose-responsive inhibition of tumor growth ranging from 25 to 200 mg/kg with once-daily dosing in an in vivo antitumor model involving PI3K-driven NCI-H1975 xenograft tumors, ^[1].
体外研究	PF-4989216 possesses outstanding PI3Kα Ki (0.6 nM), good cellular potency with S473 IC50 of 79 nM, and high selectivity against mTOR with mTOR Ki of 1440 nM. It exhibits excellent selectivity against over 40 other kinases, with minimal major CYP inhibitions. Inhibition levels of less than 30% are observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM ^[1]. The toxicity profile of PF-4989216 is evaluated across various drug-sensitive and multidrug-resistant (MDR) cancer cell lines, including those overexpressing ABCB1 or ABCG2, as well as in HEK293 cells transfected with human ABCB1 or ABCG2. PF-4989216 exhibits inhibitory effects on human colon carcinoma S1 cells and ABCG2-overexpressing subline S1-M1-80 with IC50 values of 1.11±0.09 and 6.79±1.00 μM, respectively. It also inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 with IC50 values of 2.30±0.68, 23.26±2.94, and 62.57±5.46 μM, respectively. Moreover, PF-4989216 inhibits pcDNA-HEK293, ABCB1-transfected MDR19-HEK293, and ABCG2-transfected R482-HEK293 cells with IC50 values of 0.44±0.05, 0.38±0.06, and 5.05±0.89 μM, respectively ^[2].

PF-4989216 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL

PF-4989216 技术信息

CAS号	1276553-09-3
分子式	C₁₈H₁₃FN₆OS
分子量	380.399

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 30 mg/mL(78.86 mM)，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-4989216 {[allProObj[0].p_purity_real_show]}

PF-4989216 纯度/质量文件产品仅供科研

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PF-4989216 技术信息

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p110γ	p110γ, IC50:65 nM
p110α	p110α, IC50:2 nM
p110δ	p110δ, IC50:1 nM

PF-4989216 {[allProObj[0].p_purity_real_show]}

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