Name: LEE011 (Ribociclib)
Brand: Selleck Chemicals
SKU: S7440
Rating: 5 (112 reviews)

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품질 관리

배치: 순도: 99.99%

99.99

관련 타겟	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
기타 CDK 억제제	AS2863619 Ro-3306 SEL120 (SEL120-34A) hydrochloride INX-315 Tagtociclib (PF-07104091) PF-07220060 (CDK4/6-IN-6) AZD4573 ON123300 Enitociclib (BAY 1251152) Samuraciclib (ICEC0942) hydrochloride

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
DFSP105	Growth Inhibition Assay		24 h		GI50=276 nM	25852058
Myoblast	Growth Inhibition Assay		72 h		IC50=1035 nM	25810375
IMRS	Growth Inhibition Assay		72 h		IC50=873 nM	25810375
SKNAS	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
Rh28	Growth Inhibition Assay		72 h		IC50=845 nM	25810375
Rh41	Growth Inhibition Assay		72 h		IC50=7187 nM	25810375
CW9019	Growth Inhibition Assay		72 h		IC50=9912 nM	25810375
Rh5	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
Rh30	Growth Inhibition Assay		72 h		IC50＞10000 nM	25810375
778	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
449	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP3	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP6	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LP8	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
LPS141	Growth Inhibition Assay		72 h		inhibits cell growth dose dependently	25028469
778	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
449	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
LP3	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
LP6	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
LP8	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
LPS141	Growth Inhibition Assay	3.33 μM	24 h		decreases the proportion of cells in S phase	25028469
IMR5	Growth Inhibition Assay		24 h	DMSO	IC50=126 nM	24045179
BE2C	Growth Inhibition Assay		24 h	DMSO	IC50=134 nM	24045179
1643	Growth Inhibition Assay		24 h	DMSO	IC50=147 nM	24045179
SKNSH	Growth Inhibition Assay		24 h	DMSO	IC50=148 nM	24045179
SY5Y	Growth Inhibition Assay		24 h	DMSO	IC50=154 nM	24045179
NGP	Growth Inhibition Assay		24 h	DMSO	IC50=175 nM	24045179
KELLY	Growth Inhibition Assay		24 h	DMSO	IC50=220 nM	24045179
CHP134	Growth Inhibition Assay		24 h	DMSO	IC50=273 nM	24045179
NLF	Growth Inhibition Assay		24 h	DMSO	IC50=328 nM	24045179
LAN5	Growth Inhibition Assay		24 h	DMSO	IC50=429 nM	24045179
NB69	Growth Inhibition Assay		24 h	DMSO	IC50=738 nM	24045179
SKNDZ	Growth Inhibition Assay		24 h	DMSO	IC50=801 nM	24045179
NBSD	Growth Inhibition Assay		24 h	DMSO	IC50=1900 nM	24045179
SKNF1	Growth Inhibition Assay		24 h	DMSO	IC50=3500 nM	24045179
EBC1	Growth Inhibition Assay		24 h	DMSO	IC50=6400 nM	24045179
SKNAS	Growth Inhibition Assay		24 h	DMSO	IC50＞10000 nM	24045179
NB16	Growth Inhibition Assay		24 h	DMSO	IC50＞10000 nM	24045179
RPE1	Growth Inhibition Assay		24 h	DMSO	IC50＞10000 nM	24045179
Sf21	Function assay		10 mins		Inhibition of recombinant human full length N-terminal GST-tagged CDK4/Cyclin-D3 co-expressed in baculovirus infected sf21 cells using Rb substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.013 μM.	29518312
Sf21	Function assay		10 mins		Inhibition of recombinant human full length C-terminal 6His-tagged CDK9/Cyclin-T1 co-expressed in baculovirus infected sf21 cells using PDKtide substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.197 μM.	29518312
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.2862 μM.	29407975
SEM	Antiproliferative assay		72 hrs		Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.4605 μM.	29407975
KOPN8	Antiproliferative assay		72 hrs		Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.5008 μM.	29407975
NCI-H1299	Cytotoxicity assay		72 hrs		Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 5.46 μM.	29518312
T47D	Growth inhibition assay		72 hrs		Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 6.227 μM.	28651979
T47D	Cytotoxicity assay		72 hrs		Cytotoxicity against human T47D cells assessed as reduction in cell viability after 72 hrs by CCK8 assay, IC50 = 6.23 μM.	29518312
H1299	Growth inhibition assay		72 hrs		Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 7.637 μM.	28651979
KOPN8	Apoptosis assay	0.5 uM	3 hrs		Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM after 3 hrs by Western blot analysis	29407975
KOPN8	Apoptosis assay	0.5 uM	24 hrs		Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM pre-treated with NAC for 1 hr and measured after 24 hrs by Western blot analysis	29407975
Hep3B	Cell cycle assay		24 hrs		Cell cycle arrest in human Hep3B cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
HepG2	Cell cycle assay		24 hrs		Cell cycle arrest in human HepG2 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
A549	Cell cycle assay		24 hrs		Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
NCI-H460	Cell cycle assay		24 hrs		Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
T47D	Cell cycle assay		24 hrs		Cell cycle arrest in human T47D cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
MDA-MB-231	Cell cycle assay		24 hrs		Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry	29518312
Fluc-labeled 4T1	Antitumor assay	130 mg/kg	18 days		Antitumor activity against mouse Fluc-labeled 4T1 cells implanted in Balb/c mouse assessed as reduction in tumor weight at 130 mg/kg, ip administered daily for 18 days measured after 8 to 25 days	29518312
T47D	Cell cycle assay		24 hrs		Induction of cell cycle arrest in human T47D cells assessed as increase in G0/G1 phase accumulation incubated for 24 hrs by flow cytometry	28651979
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	434.54	화학식	C₂₃H₃₀N₈O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1211441-98-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	LEE011			Smiles	CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

용해도

In vitro
배치:

DMSO : 8 mg/mL (18.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 8 mg/mL (18.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 7 mg/mL (16.1 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 22 mg/mL (50.62 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (46.02 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.100mg/ml (2.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징	Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
Targets/IC₅₀/Ki	CDK4 (Cell-free assay) 10 nM CDK6 (Cell-free assay) 39 nM
시험관 내(In vitro)	LEE011은 이중 CDK4/CDK6 억제제로서 17개 신경모세포종 세포주 중 12개 세포주의 성장을 평균 IC50 307 nM로 유의하게 억제합니다. 신경모세포종 세포주의 성장 억제는 주로 세포증식 억제적이며 G1 Cell Cycle 정지 및 세포 노화에 의해 매개됩니다.
생체 내(In vivo)	LEE011 (200 mg/kg 매일, 경구 투여)은 체중 감소나 다른 독성 징후 없이 BE2C 또는 1643 이종이식을 보유한 마우스에서 종양 성장 지연을 유의하게 유발합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/24045179/ [2] https://pubmed.ncbi.nlm.nih.gov/31482107/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP		29789630
Growth inhibition assay	Cell viability		26390342

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05843253	Not yet recruiting	High Grade Glioma\|Diffuse Intrinsic Pontine Glioma\|Anaplastic Astrocytoma\|Glioblastoma\|Glioblastoma Multiforme\|Diffuse Midline Glioma H3 K27M-Mutant\|Metastatic Brain Tumor\|WHO Grade III Glioma\|WHO Grade IV Glioma	Nationwide Children''s Hospital\|Novartis	May 30 2024	Phase 2
NCT06075758	Recruiting	Breast Cancer	Novartis Pharmaceuticals\|Novartis	March 7 2024	--
NCT05996107	Recruiting	Breast Cancer	University of Michigan Rogel Cancer Center	February 27 2024	Phase 1

기술 지원

취급 설명서

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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):

LEE011 (Ribociclib) CDK4/6 억제제

화학 구조

분자량: 434.54

품질 관리

세포 배양, 처리 및 작업 농도

화학 정보, 보관 및 안정성

용해도

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘

적용 분야

임상시험 정보

기술 지원