PD0166285

目錄號：S8148 Purity: 99.59%

PD0166285 是一種有效的 Wee1 和 Chk1 抑制劑，對Wee1和Myt1的IC50值分別為24 nM和72 nM。PD0166285 也是一種新型的G2檢查點的抑制劑。PD0166285 可誘導(dǎo)凋亡。

PD0166285 Chemical Structure

CAS: 185039-89-8

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1777.23	現(xiàn)貨
5mg	1613.55	現(xiàn)貨
25mg	5709.33	現(xiàn)貨
100mg	12858.48	現(xiàn)貨
1g	49058.75	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次： S814801 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false 純度： 99.59%

99.59

PD0166285相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Adavosertib (MK-1775)	點擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復(fù)化合物庫細(xì)胞周期化合物庫	點擊展開

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻(xiàn)信息
MCF-7	Function assay	12 mg/kg		Weight change of MCF-7 tumor cells in mice at 12 mg/kg peroral dose, days 1-15 administration	9703473
RAVSMCs	Function assay		2 hr	Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in rat aortic vascular smooth muscle cells (RAVSMCs) after 2 hr, IC50=0.0065μM	9784112
C6	Function assay		2 hr	Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in C6 rat glioma cells after 2 hr, IC50=0.005μM	9784112
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.16μM	28792760
HEK293T	Antiproliferative assay		72 hrs	Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.29μM	28792760
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.52μM	28792760
C6	Function assay			Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells, IC50=0.005μM	9703473
NIH3T3	Function assay			Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells, IC50=0.0018μM	9703473
SW-620	Function assay			Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined, IC50=0.27μM	10956222
HT-29	Function assay			Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined, IC50=0.28μM	10956222
HCT-8	Function assay			Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined, IC50=0.42μM	10956222
HEK293	Function assay			Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay, IC50=0.0072μM	22770610
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
HEK293	qHTS assay			Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki=0.0008μM	29941193
HEK293	qHTS assay			Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50=0.008μM	29941193
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生物活性

產(chǎn)品描述

靶點

Wee1 ^[1] (Cell-free assay)	Myt1 ^[1] (Cell-free assay)	Chk1 ^[1] (Cell-free assay)
24 nM	72 nM	3.4 μM

體外研究(In Vitro)
體外研究活性	PD0166285在微摩爾濃度下便可抑制Wee1的活性，它取消了G2/M期DNA損傷檢驗點、致使細(xì)胞進(jìn)入早期細(xì)胞分裂（尚未進(jìn)行DNA損傷修復(fù)）。在七種檢測到的癌細(xì)胞株上，0.5 μM的PD0166285顯著抑制放射誘導(dǎo)的Cdc2磷酸化（pTyr-15和pThr-14）。PD0166285能使細(xì)胞跳過G2/M期DNA損傷檢驗點從而誘使細(xì)胞進(jìn)入早期分裂、凋亡可用來殺死癌細(xì)胞。PD0166285對Cdc2/cyclin B沒有抑制作用，但在較高濃度下（3433 nM）可抑制Chk1。對細(xì)胞以PD0166285處理可抑制cyclin D轉(zhuǎn)錄并與微管穩(wěn)定性相關(guān)^[1]^[2]。
激酶實驗	Wee1 Mass Screening
激酶實驗	45–60 nM 全長Wee1激酶用含25 μM化合物, 20 μM ATP以及122-441 nM Cdc2/cyclin B的50 μl enzyme dilution buffer進(jìn)行孵育. 在30°C孵育30分鐘后，將包含1μM biotinylated peptide, 0.25 μCi of [γ-33P]ATP的30 μl kinase buffer(67 mM Tris (pH 8.0), 40 mM NaCl, 13 mM MgCl2, 1 mM DTT, and 0.13 mM Na3VO4)和1μM biotinylated peptide, 0.25 μCi of [γ-33P]加入反應(yīng)體系，在30°C再孵育30分鐘。通過在反應(yīng)體系中加入200 μl的stop buffer以終止反應(yīng)。2400 rpm離心15分鐘，在Wallac’s Microbeta counter對平板進(jìn)行計數(shù)。
細(xì)胞實驗	細(xì)胞系	B16小鼠黑色素瘤細(xì)胞
	濃度	0.5, 1, 2 μM
	孵育時間	4小時，24小時
	方法	B16細(xì)胞在培養(yǎng)基中培養(yǎng)過夜。予以這些細(xì)胞(0, 0.5, 1.0, or 2.0 μM)PD0166285進(jìn)行不同時間的處理，處理完后，用PBS洗滌兩次。胰蛋白酶化這些細(xì)胞并進(jìn)行細(xì)胞計數(shù)。
實驗圖片	檢測方法	檢測指標(biāo)	實驗圖片	PMID
	Western blot	p-Cdc2 / Cdc2 / Wee1 / Cyclin B		17177986
	Immunofluorescence	Wee1 / α-tubulin		17177986

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	PD0166285抑制Wee1在體內(nèi)可使U251-FM惡性膠質(zhì)瘤對輻射敏感^[3]。
動物實驗	Animal Models	攜帶移植的惡性膠質(zhì)瘤細(xì)胞的裸鼠
	Dosages	0, 20, 100, 200, or 400 μM in 100 μl
	Administration	皮下注射

參考文獻(xiàn)
[1] Wang Y, et al. Cancer Res. 2001, 61(22):8211-8217. [2] Hashimoto O, et al. BMC Cancer. 2006, 6:292. [3] Mir SE, et al. Cancer Cell. 2010, 18(3):244-257.

參考文獻(xiàn)

[1] Wang Y, et al. Cancer Res. 2001, 61(22):8211-8217.
[2] Hashimoto O, et al. BMC Cancer. 2006, 6:292.
[3] Mir SE, et al. Cancer Cell. 2010, 18(3):244-257.

化學(xué)信息&溶解度

分子量	512.43	分子式	C₂₆H₂₇Cl₂N₅O₂
CAS號	185039-89-8	SDF	Download PD0166285 SDF
Smiles	CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (195.14 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 100 mg/mL (195.14 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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