Ribociclib
Appearance- Product Name
- Ribociclib
- 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;LEE01;LEE11;CS-1001;Kisqali.;Ribociclib;LEE011, >=98%;Ribociclib-d8;Ribociclib base;LEE-011. LEE 011
- CBNumber
- CB32677045
- Molecular Formula
- C23H30N8O
- Formula Weight
- 434.54
- MOL File
- 1211441-98-3.mol
Ribociclib Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 17666
- Product name
- LEE011
- Purity
- ≥95%
- Packaging
- 25 mg
- Price
- $90
- Updated
- 2024/03/01
- Product number
- 17666
- Product name
- LEE011
- Purity
- ≥95%
- Packaging
- 50 mg
- Price
- $140
- Updated
- 2024/03/01
- Product number
- 17666
- Product name
- LEE011
- Purity
- ≥95%
- Packaging
- 500μg
- Price
- $28
- Updated
- 2023/01/06
- Product number
- 17666
- Product name
- LEE011
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $53
- Updated
- 2023/01/06
- Product number
- 17666
- Product name
- LEE011
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $40
- Updated
- 2024/03/01
Ribociclib Chemical Properties,Usage,Production
Appearance
yellow Solid
Description
LEE011 is a cyclin-
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
Protein kinase inhibitor:
Treatment of breast cancer
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.
target
CDK4
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.
Metabolism
Ribociclib is hepatically metabolised via CYP3A4 by
oxidation. Ribociclib was the main circulating drug in
plasma (44%). The major circulating metabolites included
metabolite M13 (CCI284, N-hydroxylation), M4 (LEQ803,
N-demethylation), and M1 (secondary glucuronide).
Clinical activity of ribociclib was due mainly to parent drug,
with negligible contribution from circulating metabolites.
Unchanged drug accounted for 17.3% and 12.1% of
the dose in faeces and urine, respectively. Metabolite
LEQ803 represented approximately 13.9% and 3.74%
of the administered dose in faeces and urine, respectively.
Numerous other metabolites were detected in both faeces
and urine in minor amounts (≤2.78%).
Ribociclib and its metabolites are eliminated mainly via
faeces (69.1%), with a small contribution from the renal
route (22.6%).
storage
Store at -20°C
References
1) Rader?et al.?(2013),?Dual CDK4/6 inhibition induces cell-cycle arrest and senescence in neuroblastoma; Clin. Cancer Res.?19?6173 2) Kim?et al. (2013),?LEE011: an orally bioavailable, selective small-molecule inhibitor of CDK4/6 – reactivating Rb in cancer; Mol. Cancer Ther.?12?PR02 3) Tripathy?et al.?(2017),?Ribociclib(LEE011): mechanism of action and clinical impact of this selective cyclin-dependent kinase 4/6 inhibitor in various solid tumors; Clin. Cancer Res. March 28, 201
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Raw materials
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View Lastest Price from Ribociclib manufacturers
- Product
- Ribociclib 1211441-98-3
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 1000KG
- Release date
- 2021-09-14
- Product
- Ribociclib Lee011 Powder 1211441-98-3
- Price
- US $0.00/gram
- Min. Order
- 1gram
- Purity
- 99%
- Supply Ability
- 10kg
- Release date
- 2022-02-17
- Product
- LEE011 1211441-98-3
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-27