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;LEE11;LEE01;CS-1001;Kisqali.;Ribociclib;LEE011, >=98%;Ribociclib-d8;LEE-011. LEE 011;LEE-011, Ribociclib
- CBNumber:
- CB32677045
- Molecular Formula:
- C23H30N8O
- Molecular Weight:
- 434.54
- MDL Number:
- MFCD27976795
- MOL File:
- 1211441-98-3.mol
| 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) |
| form | solid |
| pka | 8.67±0.10(Predicted) |
| 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 |
| FDA UNII | TK8ERE8P56 |
| NCI Drug Dictionary | Kisqali |
| ATC code | L01EF02 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P280-P305+P351+P338 |
Ribociclib price More Price(26)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17666 | LEE011 ≥95% | 1211441-98-3 | 25 mg | $90 | 2024-03-01 | Buy |
| Cayman Chemical | 17666 | LEE011 ≥95% | 1211441-98-3 | 50 mg | $140 | 2024-03-01 | Buy |
| Cayman Chemical | 17666 | LEE011 ≥95% | 1211441-98-3 | 500μg | $28 | 2023-01-06 | Buy |
| Cayman Chemical | 17666 | LEE011 ≥95% | 1211441-98-3 | 1mg | $53 | 2023-01-06 | Buy |
| Cayman Chemical | 17666 | LEE011 ≥95% | 1211441-98-3 | 5mg | $40 | 2024-03-01 | Buy |
Ribociclib Chemical Properties,Uses,Production
Appearance
yellow Solid
Description
LEE011 is a cyclin-
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
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
Ribociclib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 | sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9348 | 55 |
| Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 | product@chemlin.com.cn | CHINA | 3012 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 | sales@tianpharm.com | CHINA | 304 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| Shochem(Shanghai) Co.,Ltd | 86-21-50800795 | info@shochem.com | CHINA | 288 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
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View Lastest Price from Ribociclib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2022-02-18 | Ribociclib Lee011 Powder
1211441-98-3
|
US $0.00 / gram | 1gram | 99% | 10kg | Zhejiang J&C Biological Technology Co.,Limited | |
 |
2021-09-15 | Ribociclib
1211441-98-3
|
US $0.00 / KG | 1KG | 99% | 1000KG | Hangzhou Huarong Pharm Co., Ltd. | |
 |
2021-07-02 | LEE011
1211441-98-3
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd |
-
- Ribociclib Lee011 Powder
1211441-98-3
- US $0.00 / gram
- 99%
- Zhejiang J&C Biological Technology Co.,Limited
-
- Ribociclib
1211441-98-3
- US $0.00 / KG
- 99%
- Hangzhou Huarong Pharm Co., Ltd.
-
- LEE011
1211441-98-3
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd