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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
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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
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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.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17666
Product name
LEE011
Purity
≥95%
Packaging
25 mg
Price
$90
Updated
2024/03/01
Cayman Chemical
Product number
17666
Product name
LEE011
Purity
≥95%
Packaging
50 mg
Price
$140
Updated
2024/03/01
Cayman Chemical
Product number
17666
Product name
LEE011
Purity
≥95%
Packaging
500μg
Price
$28
Updated
2023/01/06
Cayman Chemical
Product number
17666
Product name
LEE011
Purity
≥95%
Packaging
1mg
Price
$53
Updated
2023/01/06
Cayman Chemical
Product number
17666
Product name
LEE011
Purity
≥95%
Packaging
5mg
Price
$40
Updated
2024/03/01
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Ribociclib Chemical Properties,Usage,Production

Appearance

yellow Solid

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

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

Ribociclib Preparation Products And Raw materials

Raw materials

Preparation Products

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Ribociclib Suppliers

Suzhou Carbonwell Pharma-Tech Co., Ltd
Tel
0512-0512-88981216 13776013740
Email
1320558046@qq.com
Country
China
ProdList
72
Advantage
58
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 17702719238
Email
sales@sun-shinechem.com
Country
China
ProdList
960
Advantage
64
Shaanxi Henghan New Materials Co., Ltd
Tel
15619311539
Email
907967238@qq.com
Country
China
ProdList
2770
Advantage
58
TIANJIN PHARMACN MEDICAL TECHNOLOGY CO.,LTD.
Tel
022-60182192,1339732154 18722583064
Fax
86-22-60979672
Email
marketing@pharmacn.com
Country
China
ProdList
112
Advantage
61
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8415
Advantage
55
Daicel Chiral Technologies (China)CO.,LTD
Tel
021-50460086-9 15921403865
Fax
+86-21-50462321
Email
han_yajun@dctc.daicel.com
Country
China
ProdList
7189
Advantage
65
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Changzhou Joyous Chemical Co., Ltd.
Tel
0519-85607258
Fax
0519-85607278
Email
sales@joyouschem.com
Country
China
ProdList
294
Advantage
60
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View Lastest Price from Ribociclib manufacturers

Hangzhou Huarong Pharm Co., Ltd.
Product
Ribociclib 1211441-98-3
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000KG
Release date
2021-09-14
Zhejiang J&C Biological Technology Co.,Limited
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
Zhuozhou Wenxi import and Export Co., Ltd
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

1211441-98-3, RibociclibRelated Search:


  • 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%
  • 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
  • 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
  • Ribociclib-d8
  • LEE-011,Ribociclib,LEE011
  • Kisqali.
  • LEE-011. LEE 011
  • LEE011; LEE-011. LEE 011; RIBOCICLIB; KISQALI.
  • 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
  • Cyclin dependent kinase,LEE 011,Ribociclib,inhibit,Inhibitor,LEE-011,CDK
  • Ribociclib base
  • 1211441-98-3
  • C23H30N8O
  • Inhibitors