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Abemaciclib mesylate

別名: LY2835219 mesylate 中文名稱(chēng)：甲磺酸阿貝西尼

Abemaciclib mesylate是一種有效的，選擇性CDK4和CDK6抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50分別為2 nM和10 nM。Phase 3。

Abemaciclib mesylate Chemical Structure

Abemaciclib mesylate Chemical Structure

CAS: 1231930-82-7

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
5mg 647.01 現(xiàn)貨
25mg 1941.03 現(xiàn)貨
100mg 4823.91 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Abemaciclib mesylate相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

CDK Signaling Pathways

CDK信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
COLO205 Inhibition of CDK4 in human 0.1 to 10 uM 24 hrs Inhibition of CDK4 in human COLO205 cells assessed as reduction in total Rb protein level at 0.1 to 10 uM after 24 hrs by immunoblotting method 29459274
COLO205 Cell cycle assay up to 10 uM 24 hrs Cell cycle arrest in human COLO205 cells assessed as accumulation at G2/M phase up to 10 uM after 24 hrs by propidium iodide staining based FACS analysis 29459274
insect cells? Function assay 50 mins Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter, IC50=2 nM 26115571
human COLO205 cells Function assay 24 h Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis 26115571
human COLO205 cells Function assay 24 h Inhibition of CDK4/6 in human COLO205 cells assessed as maximum cell cycle arrest at G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis 26115571
insect cells? Function assay 50 mins Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP, Ki=0.6 nM 26115571
HCT116 Antiproliferative assay 72 hrs IC50 = 0.54 μM 30165341
MCF7 Antiproliferative assay 72 hrs IC50 = 0.71 μM 30165341
PANC1 Antiproliferative assay 72 hrs IC50 = 5.94 μM 30165341
Sf9 Function assay 90 mins Inhibition of recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation countin, Ki = 0.002 μM. 27171036
Sf9 Function assay 90 mins Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintilla, Ki = 0.01 μM. 27171036
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay, IC50 = 0.46 μM. 29074254
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay, IC50 = 0.0481 μM. 29247857
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.0078 μM. 29429832
Sf9 Function assay 90 mins Inhibition of recombinant human full length CDK1/Cyclin D3 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay, IC50 = 0.056 μM. 29429832
MDA-MB-231 Antiproliferative activity against human 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay, IC50 = 0.191 μM. 29429832
COLO205 Antiproliferative activity against human 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay, IC50 = 0.217 μM. 29459274
MDA-MB-468 Antiproliferative activity against human 96 hrs Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay, IC50 = 4.808 μM. 29459274
Sf9 Function assay Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP, IC50 = 0.371 μM. 26741853
Sf21 Function assay Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, Ki = 3.91 μM. 27171036
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.002 μM. 29429832
Sf9 Function assay Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method, IC50 = 0.01 μM. 29429832
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生物活性

產(chǎn)品描述 Abemaciclib mesylate是一種有效的，選擇性CDK4和CDK6抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50分別為2 nM和10 nM。Phase 3。
靶點(diǎn)
CDK4 [1]
(Cell-free assay)		 CDK6 [1]
(Cell-free assay)
2 nM 10 nM
體外研究(In Vitro)
體外研究活性

LY2835219是一種口服有效的細(xì)胞周期蛋白依賴(lài)性激酶（CDK）抑制劑，靶向作用于CDK4（cyclin D1）和CDK6（cyclin D3）細(xì)胞周期通路，具有潛在的抗腫瘤活性。LY2835219特異性抑制CDK4和6，從而在早G1期抑制視網(wǎng)膜母細(xì)胞瘤（Rb）蛋白磷酸化。抑制Rb磷酸化，防止CDK-介導(dǎo)的G1-S期轉(zhuǎn)換，從而使細(xì)胞周期停滯在G1期，抑制DNA合成，且抑制癌細(xì)胞生長(zhǎng)。某些類(lèi)型的癌癥中絲/蘇氨酸激酶CDK4/6的過(guò)表達(dá)，導(dǎo)致細(xì)胞周期調(diào)節(jié)失控。[1]
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2 p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR p-Rb(S780) / Rb / p21 27748766
Growth inhibition assay Cell viability 26909611
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

LY2835219-MsOH處理腦的劑量百分比為0.5–3.9%。LY2835219-MsOH處理皮下和顱內(nèi)膠質(zhì)瘤模型（U87MG），抑制腫瘤生長(zhǎng)，這種作用存在劑量依賴(lài)性，不管是單獨(dú)處理，還是與Temozolomide聯(lián)用。[1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06139107 Recruiting
Breast Cancer
Mridula George MD|Rutgers The State University of New Jersey
 June 21 2024 Phase 1
NCT06259929 Not yet recruiting
Breast Cancer
Fondazione Oncotech
 April 1 2024 Phase 2

化學(xué)信息&溶解度

分子量 602.7 分子式

C27H32F2N8.CH4O3S
CAS號(hào) 1231930-82-7 SDF Download Abemaciclib mesylate SDF
Smiles CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F.CS(=O)(=O)O
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

Water : 100 mg/mL (165.92 mM)

DMSO : 24 mg/mL ( (39.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 13 mg/mL (21.56 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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。

技術(shù)支持

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常見(jiàn)問(wèn)題及建議解決方法

問(wèn)題 1:
Is your product S7158 LY2835219 “mesylate salt form”?

回答：
Our S7158 LY2835219 is mesylate salt form.

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