LEE011

Base Information

Chemical Name:LEE011
CAS No.:1211441-98-3
Molecular Formula:C23H30N8O
Molecular Weight:434.544
Hs Code.:
Mol file:1211441-98-3.mol

Synonyms:7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]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]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%;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

Suppliers and Price of LEE011

Supply Marketing:

Business phase:: The product has achieved commercial mass production^*data from LookChem market partment

Manufacturers and distributors:

Manufacture/Brand
Chemicals and raw materials
Packaging
price

TRC
LEE011
100mg
$ 300.00

Tocris
Ribociclib ≥98%(HPLC)
50
$ 125.00

DC Chemicals
Ribociclib(LEE011) >99%
100 mg
$ 300.00

Crysdot
Ribociclib(LEE011) 98+%
100mg
$ 666.00

Crysdot
Ribociclib(LEE011) 98+%
50mg
$ 461.00

ChemScene
Ribociclib 99.93%
10mg
$ 96.00

ChemScene
Ribociclib 99.93%
5mg
$ 72.00

ChemScene
Ribociclib 99.93%
100mg
$ 216.00

ChemScene
Ribociclib 99.93%
200mg
$ 348.00

Chemenu
7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide 98%
100mg
$ 262.00

Total 86 raw suppliers

Chemical Property of LEE011

Chemical Property:

Vapor Pressure:0-0Pa at 20-25℃
Boiling Point:730.8±70.0 °C(Predicted)
PKA:8.67±0.10(Predicted)
PSA：91.21000
Density:1.39±0.1 g/cm3(Predicted)
LogP:3.26320
Storage Temp.:-20°C
Solubility.:Soluble in DMSO (up to 10 mg/ml)

Purity/Quality:

99% ^*data from raw suppliers

LEE011 ^*data from reagent suppliers

Safty Information:

Pictogram(s):
Hazard Codes:

MSDS Files:: SDS file from LookChem

Useful:

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).
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.
Clinical Use Protein kinase inhibitor: Treatment of breast cancer
Drug interactions Potentially hazardous interactions with other drugs The concomitant use of strong CYP3A4 inhibitors including, but not limited to, the following must be avoided: clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir, ritonavir, nefazodone, nelfinavir, posaconazole, saquinavir, telaprevir, telithromycin, verapamil and voriconazole. The concomitant use of strong CYP3A4 inducers may therefore lead to decreased exposure and consequently a risk for lack of efficacy. The concomitant use of strong CYP3A4 inducers should be avoided, including, but not limited to, phenytoin, rifampicin, carbamazepine and St John's wort. Caution and monitoring for toxicity are advised during concomitant treatment with sensitive substrates of drug transporters P-gp, BCRP, OATP1B1/1B3, OCT1, OCT2, MATE1 and BSEP which exhibit a narrow therapeutic index, including but not limited to digoxin, pravastatin, rosuvastatin and metformin. Co-administration of Kisqali with medicinal products with a known potential to prolong the QT interval such as anti-arrhythmic medicinal products (including, but not limited to, amiodarone, disopyramide, procainamide, quinidine and sotalol), and other medicinal products that are known to prolong the QT interval (including, but not limited to, chloroquine, halofantrine, clarithromycin, haloperidol, methadone, moxifloxacin, pimozide and intravenous ondansetron) should be avoided.

Technology Process of LEE011

There total 1 articles about LEE011 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

: 571189-16-7
4-(6-nitropyridin-3-yl)-piperazine-1-carboxylic acid tert-butyl ester

: 1211441-98-3
(7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide)

Guidance literature:: Multi-step reaction with 3 steps

1.1: hydrogen / palladium 10% on activated carbon / water; methanol / 0.25 h / 19 - 54 °C / 1551.49 - 2327.23 Torr / Inert atmosphere

2.1: caesium carbonate / palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl / 4-methyl-2-pentanone / 3.25 h / 37 - 103 °C / Inert atmosphere

3.1: hydrogenchloride; water / toluene / 1.08 h / 9 - 28 °C / Inert atmosphere

3.2: Si-thiol functionalized silica gel / 6 h / 30 - 53 °C / pH 2.9 - 3.5

With hydrogenchloride; water; hydrogen; caesium carbonate; palladium 10% on activated carbon; palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; In methanol; water; 4-methyl-2-pentanone; toluene;