Abemaciclib (LY2835219) Mesylate

別名: LY2835219 mesylate 中文名稱：甲磺酸阿貝西尼

目錄號：S7158 Purity: 99.97%

Abemaciclib mesylate是一種有效的，選擇性CDK4和CDK6抑制劑，無細胞試驗中IC50分別為2 nM和10 nM。Phase 3。

Abemaciclib (LY2835219) Mesylate Chemical Structure

CAS: 1231930-82-7

規(guī)格	價格	庫存
10mM (1mL in DMSO)	794.43	現(xiàn)貨
5mg	647.01	現(xiàn)貨
25mg	1191	現(xiàn)貨
100mg	2370	現(xiàn)貨
1g	7944.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產品質控

批次：純度： 99.97%

99.97

Abemaciclib (LY2835219) Mesylate相關產品

相關靶點	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	點擊展開
相關產品	Ro-3306 Dinaciclib Roscovitine Flavopiridol (Alvocidib) SNS-032 (BMS-387032) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 R547 Riviciclib hydrochloride (P276-00) (E/Z)-TG003 Kenpaullone CVT-313 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) SU9516 Wogonin SEL120 (SEL120-34A) hydrochloride THZ531 PF-06873600 ON123300 LY2857785 Senexin A Samuraciclib (ICEC0942) hydrochloride NU6027 ML167 NU2058 MC180295 NSC95397 CDK2-IN-73 (CDK2-IN-4) BRD6989 HLM006474 AS2863619 Simurosertib CDKI-73	點擊展開
相關化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息(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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產品描述

Abemaciclib mesylate是一種有效的，選擇性CDK4和CDK6抑制劑，無細胞試驗中IC50分別為2 nM和10 nM。Phase 3。

靶點

CDK4 ^[1] (Cell-free assay)	CDK6 ^[1] (Cell-free assay)
2 nM	10 nM

體外研究(In Vitro)
體外研究活性	LY2835219是一種口服有效的細胞周期蛋白依賴性激酶（CDK）抑制劑，靶向作用于CDK4（cyclin D1）和CDK6（cyclin D3）細胞周期通路，具有潛在的抗腫瘤活性。LY2835219特異性抑制CDK4和6，從而在早G1期抑制視網(wǎng)膜母細胞瘤（Rb）蛋白磷酸化。抑制Rb磷酸化，防止CDK-介導的G1-S期轉換，從而使細胞周期停滯在G1期，抑制DNA合成，且抑制癌細胞生長。某些類型的癌癥中絲/蘇氨酸激酶CDK4/6的過表達，導致細胞周期調節(jié)失控。^[1]
實驗圖片	檢測方法	檢測指標	實驗圖片	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

體內研究(In Vivo)
體內研究活性	LY2835219-MsOH處理腦的劑量百分比為0.5–3.9%。LY2835219-MsOH處理皮下和顱內膠質瘤模型（U87MG），抑制腫瘤生長，這種作用存在劑量依賴性，不管是單獨處理，還是與Temozolomide聯(lián)用。^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
https://pubmed.ncbi.nlm.nih.gov/29497278/ https://pubmed.ncbi.nlm.nih.gov/33495604/ https://pubmed.ncbi.nlm.nih.gov/32929370/

參考文獻

https://pubmed.ncbi.nlm.nih.gov/29497278/
https://pubmed.ncbi.nlm.nih.gov/33495604/
https://pubmed.ncbi.nlm.nih.gov/32929370/

化學信息&溶解度

分子量	602.7	分子式	C₂₇H₃₂F₂N₈.CH₄O₃S
CAS號	1231930-82-7	SDF	Download Abemaciclib (LY2835219) 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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

Water : 100 mg/mL (165.92 mM)

DMSO : 24 mg/mL ( (39.82 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 13 mg/mL (21.56 mM)

Water : 100 mg/mL (165.92 mM)

DMSO : 83 mg/mL ( (137.71 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 24 mg/mL (39.82 mM)

Water : 100 mg/mL (165.92 mM)

Ethanol : 100 mg/mL (165.92 mM)

DMSO : 33 mg/mL ( (54.75 mM) Warmed with 50°C water bath; Ultrasonicated; ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 100 mg/mL (165.92 mM)

DMSO : 33 mg/mL ( (54.75 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 4 mg/mL (6.63 mM)

摩爾濃度計算器

體內溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動物體內配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 Corn oil 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	0.150mg/ml (0.25mM)	以 1 mL 工作液為例，取50μL3mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術支持

在訂購、運輸、儲存和使用我們的產品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時內盡快聯(lián)系您。

操作手冊

如果有其他問題，請給我們留言。

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常見問題及建議解決方法

問題 1:
Is your product S7158 “mesylate salt form”?

回答：
It is the mesylate salt form of our S7158 LY2835219.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Abemaciclib (LY2835219) Mesylate

產品質控

Abemaciclib (LY2835219) Mesylate相關產品

相關信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

技術支持

常見問題及建議解決方法