Abemaciclib
别名: LY2835219 中文名称：玻玛西林,阿贝西利
Abemaciclib是一种对 CDK4/6 有选择性的细胞周期抑制剂，在无细胞试验中的IC50值分别为2 nM和10 nM。
Abemaciclib Chemical Structure
CAS: 1231929-97-7
产品质控
批次：
纯度：
99.90%
99.90
常与Abemaciclib一起在实验中被使用的化合物
Abemaciclib和Palbociclib HCl是CDK4/6抑制剂，可抑制AT2和NKX2-5细胞中的SARS-CoV-2复制。
Rudraraju R, et al. Stem Cell Reports. 2023 Jun 13;18(6):1308-1324.
Abemaciclib和Ribociclib已获得FDA批准，可与芳香酶抑制剂或氟维司群等内分泌疗法一起作为乳腺癌治疗的选择。
Ademaciclib和Olaparib联合治疗在C4–2b、C4–2b-ENZR和NCI-H660模型中增加了sub-G1细胞的百分比。
Abemaciclib与Trametinib可协同降低RAS突变RMS细胞系RD的存活率。
在宫颈癌小鼠模型中，与单独使用Paclitaxel相比，Abemaciclib和Paclitaxel可有效抑制肿瘤生长。
Liu Y, et al. Fundam Clin Pharmacol. 2021 Feb;35(1):156-164.
Abemaciclib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Abemaciclib是一种对 CDK4/6 有选择性的细胞周期抑制剂，在无细胞试验中的IC50值分别为2 nM和10 nM。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 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 |
化学信息&溶解度
| 分子量 | 506.59 | 分子式 | C27H32F2N8 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
Ethanol : 11 mg/mL (21.71 mM) DMSO : 4 mg/mL ( (7.89 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy Abemaciclib | Abemaciclib supplier | purchase Abemaciclib | Abemaciclib cost | Abemaciclib manufacturer | order Abemaciclib | Abemaciclib distributor
