Abemaciclib methanesulfonate|1231930-82-7|(LY2835219 methanesulfonate)-陌孚医药/Medlife

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Abemaciclib methanesulfonate (Synonyms: LY2835219 methanesulfonate)

目录号: PL04606 纯度: ≥99%

CAS No. :1231930-82-7

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中文名称	Abemaciclib methanesulfonate
中文别名	N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-异丙基-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸盐;2-二甲胺基甲基苯酚;LY2835219 抑制剂;LY2835219甲磺酸盐;N-(5-((4-甲基哌嗪-1-基甲基)吡啶-2-基)-5氟-4-(4-氟-1-异丙基-2-甲基-1H-苯并[D]咪唑-6-基)嘧啶-2-胺甲磺酸盐;N-[5-[(4-乙基-1-哌嗪)甲基]-2-吡啶]-5-氟-4-[4-氟-2-甲基-1-(1-甲基乙基)-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸盐;甲磺酸盐;阿贝西利甲磺酸盐
英文名称	Abemaciclib methanesulfonate
英文别名	N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine Methanesulfonate;LY2835219;abemaciclib (LY2835219);Bemaciclib;N-(5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine methanesulfonate;N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]...;N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyr;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;6 dual inhibitor;ABEMACICLIB;CDK4;CS-1229;LY-2835219;QCR-274;Bemaciclib(salt);Abemaciclib methanesulfonate
Cas No.	1231930-82-7
分子式	C₂₇H₃₂N₈F₂^.CH₄O₃S
分子量	602.70
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) 是选择性的 CDK4/6 抑制剂，抑制 CDK4/CDK6 的 IC₅₀ 分别为 2 nM 和 10 nM。

生物活性

Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC 50 s of 2 nM and 10 nM for CDK4 and CDK6, respectively.

性状

Solid

IC50 & Target[1][2]

Cdk4/cyclin D1 2 nM (IC50) CDK6/cyclinD1 1

体外研究(In Vitro)

Abemaciclib (LY2835219) reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells. Abemaciclib (LY2835219) shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively. Abemaciclib (LY2835219) 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. has not independently confirmed the accuracy of these methods. They are for refe

体内研究(In Vivo)

Abemaciclib (LY2835219) (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Ku BM, et al. 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.
[2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

溶解度数据	In Vitro: H₂O : 125 mg/mL (207.40 mM; Need ultrasonic)DMSO : 10 mg/mL (16.59 mM; ultrasonic and warming and heat to 80°C)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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