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Abemaciclib
別名: LY2835219 中文名稱：?，斘髁?阿貝西利
Abemaciclib是一種對 CDK4/6 有選擇性的細胞周期抑制劑，在無細胞試驗中的IC50值分別為2 nM和10 nM。
Abemaciclib Chemical Structure
CAS: 1231929-97-7
產(chǎn)品質(zhì)控
批次：
純度：
99.90%
99.90
常與Abemaciclib一起在實驗中被使用的化合物
Abemaciclib和Palbociclib HCl是CDK4/6抑制劑，可抑制AT2和NKX2-5細胞中的SARS-CoV-2復制。
Rudraraju R, et al. Stem Cell Reports. 2023 Jun 13;18(6):1308-1324.
Abemaciclib和Ribociclib已獲得FDA批準，可與芳香酶抑制劑或氟維司群等內(nèi)分泌療法一起作為乳腺癌治療的選擇。
Ademaciclib和Olaparib聯(lián)合治療在C4–2b、C4–2b-ENZR和NCI-H660模型中增加了sub-G1細胞的百分比。
Abemaciclib與Trametinib可協(xié)同降低RAS突變RMS細胞系RD的存活率。
在宮頸癌小鼠模型中，與單獨使用Paclitaxel相比，Abemaciclib和Paclitaxel可有效抑制腫瘤生長。
Liu Y, et al. Fundam Clin Pharmacol. 2021 Feb;35(1):156-164.
Abemaciclib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 |
|---|---|---|---|---|---|
| COLO205 | Function assay | 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 arrest 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 |
| MHH-ES-1 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| CHLA-258 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-3 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-1 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| RD-ES | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| A673 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| TC-71 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-7 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| Cado-ES-1 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| SK-ES-1 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| 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, IC50=0.12 μM | 26115571 | |
| ES-8 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| EW8 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-6 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-2 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| SMS-CTR | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| ES-4 | Proliferation assay | 96 hours | antiproliferative effects with an absolute EC50 value below 1 μmol/L | 30131386 | |
| CT26 | Cell viability assay | 96 hours | IC50=2.7 μM | 29539425 | |
| 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 = 0.0006 μM. | 26115571 | |
| 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 = 0.002 μM. | 26115571 | |
| COLO205 | Function assay | 24 hrs | 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, INH = 6.7 μM. | 26115571 | |
| 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 assay | 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 assay | 96 hrs | Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay, IC50 = 0.217 μM. | 29459274 | |
| MDA-MB-468 | Antiproliferative assay | 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Abemaciclib是一種對 CDK4/6 有選擇性的細胞周期抑制劑，在無細胞試驗中的IC50值分別為2 nM和10 nM。 | ||||
|---|---|---|---|---|---|
| 靶點 |
|
| 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 |
化學信息&溶解度
| 分子量 | 506.59 | 分子式 | C27H32F2N8 |
| CAS號 | 1231929-97-7 | 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 | ||
| 儲存條件(自收到貨起) | 3年 -20°C 粉狀 | ||
|
體外溶解度 |
Ethanol : 11 mg/mL (21.71 mM) DMSO : 4 mg/mL ( (7.89 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 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
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
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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