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Abemaciclib mesylate
别名: LY2835219 mesylate 中文名称：甲磺酸阿贝西尼
Abemaciclib mesylate是一种有效的，选择性CDK4和CDK6抑制剂，无细胞试验中IC50分别为2 nM和10 nM。Phase 3。
Abemaciclib mesylate Chemical Structure
CAS: 1231930-82-7
产品质控
批次：
纯度：
99.97%
99.97
Abemaciclib mesylate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(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Abemaciclib mesylate是一种有效的，选择性CDK4和CDK6抑制剂，无细胞试验中IC50分别为2 nM和10 nM。Phase 3。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | LY2835219是一种口服有效的细胞周期蛋白依赖性激酶（CDK）抑制剂，靶向作用于CDK4（cyclin D1）和CDK6（cyclin D3）细胞周期通路，具有潜在的抗肿瘤活性。LY2835219特异性抑制CDK4和6，从而在早G1期抑制视网膜母细胞瘤（Rb）蛋白磷酸化。抑制Rb磷酸化，防止CDK-介导的G1-S期转换，从而使细胞周期停滞在G1期，抑制DNA合成，且抑制癌细胞生长。某些类型的癌症中丝/苏氨酸激酶CDK4/6的过表达，导致细胞周期调节失控。[1] |
|||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-Rb(S780) / Rb / p21 p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2 |
|
26909611 | |
| Growth inhibition assay | Cell viability |
|
26909611 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | LY2835219-MsOH处理脑的剂量百分比为0.5–3.9%。LY2835219-MsOH处理皮下和颅内胶质瘤模型（U87MG），抑制肿瘤生长，这种作用存在剂量依赖性，不管是单独处理，还是与Temozolomide联用。[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 |
|
化学信息&溶解度
| 分子量 | 602.7 | 分子式 | C27H32F2N8.CH4O3S |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
Water : 100 mg/mL (165.92 mM) DMSO : 24 mg/mL ( (39.82 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 13 mg/mL (21.56 mM) |
摩尔浓度计算器 |
|
体内溶解配方 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。
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常见问题及建议解决方法
问题 1:
Is your product S7158 LY2835219 “mesylate salt form”?
回答：
Our S7158 LY2835219 is mesylate salt form.
