LY2835219

Name: LY2835219
SKU: GC16822
Availability: InStock
Rating: 5 (30 reviews)

(Synonyms: Abemaciclib; LY2835219 methanesulfonate) 目录号 : GC16822

LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂，在非细胞实验中的 IC₅₀ 分别为 2nM 和 10nM。

LY2835219 Chemical Structure

Cas No.:1231930-82-7

规格价格库存购买数量

10mM (in 1mL DMSO)	¥675.00	现货
5mg	¥540.00	现货
25mg	¥1,125.00	现货
100mg	¥1,350.00	现货

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Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

客户使用产品发表文献 1 篇

Drug Resist Update (2024)：101161.

产品文档

Quality Control & SDS

View current batch:

Purity: >99.00%

实验参考方法

Cell experiment [1]:
Cell lines	Colo-205 colorectal cells
Preparation Method	Colo-205 colorectal cells treated with LY2835219 free base (0.001-10μM) for 24h.
Reaction Conditions	LY2835219 free base: 0.001-10μM; 24h
Applications	LY2835219 free base treated with Colo-205 colorectal cells showed a concentration-dependent inhibition of p-Rb and a corresponding arrest of cells in G1 (2 N DNA content), resulting in a decreased number of cells due to inhibition of proliferation.
Animal experiment [2]:
Animal models	Colo-205 human xenograft tumor model
Preparation Method	LY2835219 free base was formulated in 1 % hydroxyethyl cellulose + 0.1 % antifoam in 25mM PBS pH 2 and administered orally by gavage (final volume 0.2 mL) at the indicated dose and schedule.
Dosage form	LY2835219 free base (50mg/kg; po; 56d)
Applications	LY2835219 free base is effective and well tolerated when administered up to 56 days in Colo-205 human xenograft tumor mice without significant loss of body weight or tumor outgrowth.
References: [1]. Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. 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.

产品描述

LY2835219 free base is a potent and selective inhibitor of CDK4 and CDK6 with IC₅₀ of 2nM and 10nM in cell-free assays, respectively^[1].

LY2835219 free base (0.001-10μM; 24h) inhibited p-Rb in a concentration-dependent manner, resulting in cell arrest in the G1 phase (2 N DNA content) and a decrease in cell number due to inhibition of proliferation. LY2835219 free base inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells^[2]. LY2835219 free base (0.1, 0.2 and 0.4μM; 24h) potentiated the cytotoxicity of conventional chemotherapeutic agents in ABCB1 and ABCG2-overexpressing cells^[3].

LY2835219 free base (50mg/kg; po; 56d) was effective and well tolerated in mice bearing Colo-205 xenograft tumors. After administration for up to 56days, there was no significant weight loss in mice and no significant tumor growth^[2]. LY2835219 free base (45mg/kg; po; 14d) combined with RAD001 had a synergistic anti-tumor effect on HNSCC xenograft tumors[4].

References:
[1].Corona SP, Generali D. Abemaciclib: a CDK4/6 inhibitor for the treatment of HR+/HER2- advanced breast cancer. Drug Des Devel Ther. 2018 Feb 16;12:321-330.
[2]. Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. 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.
[3]Wu T, Chen Z, To KKW, Fang X, Wang F, Cheng B, Fu L. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.
[4]. Ku BM, Yi SY, Koh J, Bae YH, Sun JM, Lee SH, Ahn JS, Park K, Ahn MJ. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13.

LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂，在非细胞实验中的 IC₅₀ 分别为 2nM 和 10nM^[1]。

LY2835219 free base（0.001-10μM，24h）以浓度依赖性方式抑制 p-Rb，导致细胞停滞在 G1 期（2 N DNA 含量），细胞数量因增殖受抑制而减少。LY2835219 free base以低纳摩尔的效价抑制 CDK4 和 CDK6，抑制 Rb 磷酸化，导致 G1 期停滞和增殖抑制，其活性对 Rb 细胞具有特异性^[2]。LY2835219 free base（0.1、0.2 和 0.4μM；24h）可增强传统化疗药物对 ABCB1 和 ABCG2 基因敲除细胞的细胞毒性^[3]。

LY2835219 free base （50mg/kg；po；56d）对 Colo-205 异种移植肿瘤小鼠有效且耐受性良好，给药长达 56 天，小鼠体重无明显下降，肿瘤无明显生长^[2]。LY2835219 free base（45mg/kg；po；14d）与 RAD001 联用对 HNSCC 异种移植瘤有协同抗肿瘤作用^[4]。

Chemical Properties

Cas No.	1231930-82-7	SDF
别名	Abemaciclib; LY2835219 methanesulfonate
化学名	N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine;methanesulfonic acid
Canonical 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
分子式	C₂₇H₃₂F₂N₈.CH₄O₃S	分子量	602.7
溶解度	≥ 30.15mg/mL in DMSO	储存条件	Store at -20°C
General tips	请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。
Shipping Condition	评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。

溶解性数据

制备储备液
		1 mg	5 mg	10 mg
	1 mM	1.6592 mL	8.296 mL	16.592 mL
	5 mM	0.3318 mL	1.6592 mL	3.3184 mL
	10 mM	0.1659 mL	0.8296 mL	1.6592 mL

摩尔浓度计算器
稀释计算器
分子量计算器

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）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

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GLPBIO为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % saline

计算重置

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GLPBIO）；

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 saline，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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。