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Ribociclib

Ribociclib Structure
CAS No.
1211441-98-3
Chemical Name:
Ribociclib
Synonyms
7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide;LEE11;LEE01;CS-1001;Kisqali.;Ribociclib;LEE011, >=98%;Ribociclib-d8;Ribociclib base;LEE-011. LEE 011
CBNumber:
CB32677045
Molecular Formula:
C23H30N8O
Molecular Weight:
434.54
MOL File:
1211441-98-3.mol
Modify Date:
2024/5/27 13:35:05

Ribociclib Properties

Boiling point 730.8±70.0 °C(Predicted)
Density 1.39±0.1 g/cm3(Predicted)
vapor pressure 0-0Pa at 20-25℃
storage temp. -20°C
solubility Soluble in DMSO (up to 10 mg/ml)
pka 8.67±0.10(Predicted)
form solid
color Off-white
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
LogP -0.8-2.3 at 20℃ and pH4-11

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338

Ribociclib Chemical Properties,Uses,Production

Description

LEE011 is a cyclin-dependent kinase (CDK) inhibitor that targets cyclin D1/CDK4 and cyclin D3/CDK6 at nanomolar concentrations. It inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth. LEE011 has been shown to reduce proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis (mean IC50 = 306 nM in sensitive lines).

Characteristics

Class: serine/threonine protein kinase
Treatment: Breast cancer
Oral bioavailability = 66%
Elimination half-life = 32 h
Protein binding = 70%

Uses

LEE 011 can be used in biological study of kinome-wide RNA interference screen reveals a role for PDK1 in acquired resistance to CDK4/6 inhibition in ER-positive breast cancer.

Mechanism of action

Ribociclib is a dual cdk4/cdk6 inhibitor. Induces G1 phase cell cycle arrest and senescence in neuroblastoma cell lines (IC50 = 306 nM). Delays tumor growth in vivo.

Clinical Use

Ribociclib was first approved in 2017 as the second CDK4/6 (cyclin-dependent kinase) inhibitor in combination with aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor positive (HR+), human epidermal growth factor receptor-2 negative (HER2?) advanced or metastatic breast cancer. In 2018, its label was expanded to pre/perimenopausal women with HR+/HER2? advanced or metastatic breast cancer.

Ribociclib Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 226)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Dr. Reddy's Laboratories Ltd +91-4049002900 +91-4049002900 Hyderabad, India 165 58 Inquiry
CDYMAX +91-9019317788 +91-9019317788 Bangalore, India 28 58 Inquiry
Vachichem +91-9886704423 +91-9880599557 Karnataka, India 72 58 Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
Hangzhou FandaChem Co.,Ltd. 008657128800458; +8615858145714 China 9337 55 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32836 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29888 58 Inquiry

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7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide 7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide LEE 011 LEE 011 7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide LEE011, >=98% 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE LEE-011, Ribociclib 7H-Pyrrolo[2,3-d]pyrimidine-6-carboxamide, 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]- Ribociclib 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidi Ribociclib Ribociclib USP/EP/BP Ribociclib Lee011 Powder LEE11 7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide 7H-Pyrrolo[2,3-d]pyrimidine-6-carboxamide, 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyri LEE01 CS-1001 LEE 011; LEE-011;RIBOCICLIB;LEE011 Ribociclib-d8 LEE-011,Ribociclib,LEE011 Kisqali. LEE-011. LEE 011 LEE011; LEE-011. LEE 011; RIBOCICLIB; KISQALI. 7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide Cyclin dependent kinase,LEE 011,Ribociclib,inhibit,Inhibitor,LEE-011,CDK Ribociclib base 1211441-98-3 C23H30N8O Inhibitors