Abemaciclib methanesulfonate | CDK | AmBeed-信号通路专用抑制剂

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Abemaciclib methanesulfonate {[allProObj[0].p_purity_real_show]}

货号：A144902

Abemaciclib methanesulfonate 是一种选择性的 CDK4/6 抑制剂，对 CDK4/6 具有高亲和力，抑制 CDK4/CDK6 的 IC50 分别为 2 nM 和 10 nM。Abemaciclib methanesulfonate 具有抗肿瘤作用，主要用于乳腺癌和其他 CDK4/6 依赖型癌症的研究和治疗。

Abemaciclib methanesulfonate 化学结构
CAS号：1231930-82-7

Abemaciclib methanesulfonate 3D分子结构
CAS号：1231930-82-7

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Abemaciclib methanesulfonate 纯度/质量文件产品仅供科研

货号：A144902 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			99%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Abemaciclib methanesulfonate 生物活性

描述

CDK4/6, forming a complex with its partner Cyclin D1/2/3, can mediate the phosphorylation of Rb in G1 cell cycle, as well as stimulating the synthesis cyclin E and D-type cyclins controlled by extracellular mitogens^[1]. LY2835219 (abemaciclib) can selectively inhibit CDK4/cyclin D1 and CDK6/cyclin D1 with IC50 values of 2 nM and 10 nM (measured by enzymatic assays), respectively. Treatment with LY2835219 for 24h showed a dose-dependent inhibition of pRb-S780, with IC50 of 120 nM, and G1 arrest with EC50 of 72 nM in Colo-205 colorectal cells. Similar effect can also be observed in MCF10A and MV4-11 AML cells. LY2835219 showed the good pharmacodynamics. Oral dose>12.5 mg/kg for 24h can decrease the level of p-Rb (a phenotypic marker for cells in G1 and CDK4/6 inhibition), topisomerase II alpha (a marker for cells in S phase) and pHH3 (a marker for cells in M phase) in mice bearing colo-205 human xenografts. Oral treatment of LY2835219 on dose of 25 - 100 mg/kg for 21 days significantly inhibited the growth of colo-205 and MV4-11 xenograft mice^[2]. There are 10 ongoing clinical trials using LY2835219 as a single agent or in combination for the treatment of tumors including breast, lung cancer, lymphoma and MCL, Stage IV NSCLC with a detectable KRAS mutation and breast cancer^[3].

作用机制

LY2835219 is a competitive ATP CDK4/6 inhibitor^[2].

Abemaciclib methanesulfonate 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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
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

Abemaciclib methanesulfonate 动物研究

Dose

Mice^[4] (s.c.): min = 12.5 mg/kg, max = 100 mg/kg

Administration

s.c.

Pharmacokinetics

Animal	Rats^[5]
Dose	40 mg/kg
Administration	o.p.
C_max	789 ng/ml
T_1/2	10.3 h
AUC_0-48h	22000
F	0.595

Abemaciclib methanesulfonate 参考文献

[1]Roskoski R Jr, et al. Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs. Pharmacol Res. 2016 May;107:249-275.

[2], et al. Symposium on the use of sinusoidally modulated light for the study of visual mechanisms in normal subjects, patients and animals (dogs). Electroencephalogr Clin Neurophysiol. 1967 Dec;23(6):586-7.

[3]Aleem E, Arceci RJ, et al. Targeting cell cycle regulators in hematologic malignancies. Front Cell Dev Biol. 2015 Apr 9;3:16.

[4]Gelbert LM, Cai S, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Oct;32(5):825-37.

[5]208716Orig1s000MultidisciplineR

Abemaciclib methanesulfonate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.30mL

1.66mL

0.83mL

16.59mL

3.32mL

1.66mL

Abemaciclib methanesulfonate 技术信息

CAS号	1231930-82-7
分子式	C₂₈H₃₆F₂N₈O₃S
分子量	602.699

别名
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解度

DMSO: 9 mg/mL(14.93 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 120 mg/mL(199.1 mM)，配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 40 mg/mL suspension

Abemaciclib methanesulfonate {[allProObj[0].p_purity_real_show]}

Abemaciclib methanesulfonate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Abemaciclib methanesulfonate 质控信息

Abemaciclib methanesulfonate 生物活性

Abemaciclib methanesulfonate 细胞研究

Abemaciclib methanesulfonate 动物研究

Abemaciclib methanesulfonate 参考文献

Abemaciclib methanesulfonate 实验方案

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Abemaciclib methanesulfonate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Abemaciclib methanesulfonate 质控信息

Abemaciclib methanesulfonate 生物活性

Abemaciclib methanesulfonate 细胞研究

Abemaciclib methanesulfonate 动物研究

Abemaciclib methanesulfonate 参考文献

Abemaciclib methanesulfonate 实验方案

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Abemaciclib methanesulfonate 纯度/质量文件产品仅供科研