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LY3009120

別名: DP-4978

LY03009120 (DP-4978)是一種有效的泛Raf抑制劑,在A375細胞中對A-raf,B-Raf,和 C-Raf的IC50分別為44 nM,31-47 nM,和 42 nM。LY03009120 可誘導(dǎo)自噬。Phase 1。

LY3009120 Chemical Structure

LY3009120 Chemical Structure

CAS: 1454682-72-4

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1466.01 現(xiàn)貨
5mg 1207.33 現(xiàn)貨
25mg 3906.82 現(xiàn)貨
100mg 8154.89 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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LY3009120相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
HCT116 Function assay <100 nM Paradoxical activation of RAS/RAF/MEK signaling pathway in human HCT116 cells expressing wild type BRAF assessed as ERK phosphorylation at <100 nM 25965804
A375 Function assay 15 mins Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.042μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.039μM. 25965804
A375 Function assay 72 hrs Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay, IC50=0.037μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.031μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.02μM. 25965804
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay, IC50=0.0092μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.044μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.061μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.091μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.098μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.1μM. 25965804
HCT116 Antiproliferative assay 67 hrs Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay, IC50=0.22μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.29μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.31μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.38μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.39μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.45μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.47μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.8μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.97μM. 25965804
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.1μM. 30529543
SK-MEL-2 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.2μM. 30529543
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.3μM. 30529543
SW579 Antiproliferative assay 72 hrs Antiproliferative activity against human SW579 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.9μM. 30529543
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.9μM. 30529543
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay, IC50=2.6μM. 30529543
HCT116 Function assay Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA, IC50=0.15μM. 25965804
A375 Function assay In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as plasma concentration required to inhibit ERK phosphorylation by 50%, INH=0.165μM. 25965804
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to B-Raf in human A375 cells by MS analysis, IC50=0.031μM. 30529543
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to C-Raf in human A375 cells by MS analysis, IC50=0.042μM. 30529543
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to A-Raf in human A375 cells by MS analysis, IC50=0.044μM. 30529543
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生物活性

產(chǎn)品描述 LY03009120 (DP-4978)是一種有效的泛Raf抑制劑,在A375細胞中對A-raf,B-Raf,和 C-Raf的IC50分別為44 nM,31-47 nM,和 42 nM。LY03009120 可誘導(dǎo)自噬。Phase 1。
靶點
C-Raf [1]
(Cell-free assay)
BRAF(V600E) [1]
(Cell-free assay)
BRAF WT [1]
(Cell-free assay)
4.3 nM 5.8 nM 15 nM
體外研究(In Vitro)
體外研究活性 LY3009120抑制A375和 HCT116細胞的生長,IC50分別為9.2和220 μM。LY3009120抑制酪氨酸激酶KDR,IC50為3.9 μM。[1]
激酶實驗 使用KiNativ試驗測定激酶活性
化合物在A375細胞裂解物中使用基于ATP的探針在5 μM下篩選。IC50值以微摩爾單位表示。細胞沉淀重懸浮在4體積裂解緩沖液[25 mM Tris pH 7.6,150 mM NaCl,1% CHAPS,1% Tergitol NP-40 型,1% v/v 磷酸酶抑制劑混合物II]中,使用尖端超聲波儀聲處理,并均質(zhì)化。裂解產(chǎn)物通過100,000 g下離心分離30分鐘除去。澄清的裂解液通過0.22 μM注射過濾器和凝膠過濾到反應(yīng)緩沖液[20 mM Hepes pH 7.8,150 mM NaCl,0.1% triton X-100,1% v/v 磷酸酶抑制劑混合物II]。抑制劑處理和探針標記之前,將終濃度為20 mM 的MnCl2加入裂解液。用于IC50測定的終抑制劑濃度為10,1,0.1,和 0.01 μM。ATP競爭性實驗在1,000,100,10,和1 μM ATP下進行。所有抑制劑的處理在室溫下進行。
細胞實驗 細胞系 A375 和 HCT116 細胞
濃度 0.51 μM
孵育時間 67 h
方法 簡而言之,細胞在DMEM高濃度葡萄糖中生長,用10%胎牛血清和1%青霉素/鏈霉素/L-谷氨酰胺增補,在37℃,5% CO2,和95%濕度下培育。允許細胞擴增到70-95%的融合度。連續(xù)稀釋的測試化合物分配加入到384孔黑色透明底板。每孔加入包含625個細胞的50 μL完全生長培養(yǎng)基。板在37℃,5% CO2,和95%濕度下培育67小時。然后,10 μL包含440 μM 刃天青的PBS溶液加入板的每孔中,板在37℃,5% CO2,和95%濕度下再培育5小時。板在Synergy2閱讀器上使用540 nm激發(fā)波長和600 nm發(fā)射波長讀取。得到的數(shù)據(jù)使用Prism軟件分析以計算IC 50值。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot Beclin-1 / Mcl-1 / LC3 / p62 p-EGFR / EGFR / p-BRAF / BRAF / p-CRAF / CRAF / p-MEK / MEK / p-AKT / AKT 28382170
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在負荷BRAF V600E ST019VR PDX腫瘤的大鼠體內(nèi),LY3009120 (15 or 30 mg/kg, p.o.)劑量依賴性抑制腫瘤生長。在負荷A375異種移植物的裸鼠體內(nèi),LY3009120 (3到50 mg/kg, p.o.)單劑量口服治療劑量依賴性抑制磷酸-ERK,4.36 mg/kg劑量下抑制50%磷酸- ERK (EC50),68.9 ng/mL或165 nM血漿濃度下達到50%磷酸- ERK (EC50) 抑制率。[1]
動物實驗 Animal Models 負荷BRAF V600E ST019VR PDX腫瘤的雌性 NIH裸鼠
Dosages 30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02014116 Terminated
Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms
Eli Lilly and Company
November 26 2013 Phase 1

化學(xué)信息&溶解度

分子量 424.51 分子式

C23H29FN6O

CAS號 1454682-72-4 SDF Download LY3009120 SDF
Smiles CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F
儲存條件(自收到貨起)

體外溶解度
批次:

DMSO : 20 mg/mL ( (47.11 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

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)

mg/kg g μL

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,: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: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: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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常見問題及建議解決方法

問題 1:
I am trying to figure out solubility of the drug LY3009120 Catalog #7842 for in vivo studies. I need some details on the formulation and how it is made to dissolve the chemical?

回答:
It can dissolve in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 1 mg/ml clearly, and in 0.5% CMC Na at 30 mg/ml as a suspension.

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