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Ribociclib

Catalog No. T6199 CAS 1211441-98-3

Synonyms: LEE011

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50：10/39 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Ribociclib, CAS 1211441-98-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 36.00
5 mg	In stock	$ 58.00
10 mg	In stock	$ 78.00
25 mg	In stock	$ 98.00
50 mg	In stock	$ 118.00
100 mg	In stock	$ 177.00
500 mg	In stock	$ 443.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 100%

Purity: 99.96%

Purity: 99.85%

Purity: 99.02%

Purity: 98.27%

Biological Description

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Description	Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50：10/39 nM).
Targets&IC50	VEGFR6:39 nM, VEGFR4:10nM
In vitro	LEE011 (200 mg/kg/day, p.o.) significantly delayed the growth of BE2C or 1643 cells in mice without causing weight loss or other toxic symptoms.
In vivo	LEE011 inhibits the growth of neuroblastoma cells, a process regulated by G1 cell cycle arrest and cellular senescence. It demonstrates significant growth suppression in 12 out of 17 neuroblastoma types evaluated, with an average IC50 of 307 nM.
Kinase Assay	Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].
Cell Research	A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. (Only for Reference)

Synonyms	LEE011
Molecular Weight	434.54
Formula	C23H30N8O
CAS No.	1211441-98-3

Storage

store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (115.06 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182. 2. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

Citations

1. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library EMA Approved Drug Library Kinase Inhibitor Library Inhibitor Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ribociclib 1211441-98-3 Angiogenesis Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors VEGFR CDK Cyclin dependent kinase inhibit Inhibitor LEE 011 LEE011 LEE-011 inhibitor

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