LEE011 (hydrochloride)
LEE011 (hydrochloride) Basic information
- Product Name:
- LEE011 (hydrochloride)
- Synonyms:
-
- LEE011 (hydrochloride)
- 7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide hydrochloride (1:1)
- LEE-011 HCl salt, Ribociclib HCl salt
- Ribociclib (Hydrochloride)
- Ribociclib HCl
- LEE011 HCl
- 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide hydrochloride
- RIBOCICLIB HYDROCHLORIDE (LEE011 HYDROCHLORIDE)
- CAS:
- 1211443-80-9
- MF:
- C23H31ClN8O
- MW:
- 470.99824
- Mol File:
- 1211443-80-9.mol
LEE011 (hydrochloride) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- H2O : 10 mg/mL (21.23 mM; Need ultrasonic)DMSO : 7.69 mg/mL (16.33 mM; Need ultrasonic)
- form
- Powder
- color
- Off-white to yellow
LEE011 (hydrochloride) Usage And Synthesis
Uses
Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
in vivo
CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment[2].
IC 50
CDK4: 10 nM (IC50); CDK6: 39 nM (IC50)
References
[1] VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. DOI:10.1158/1078-0432.CCR-14-0816
[2] Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. DOI:10.1158/1078-0432.CCR-13-1675
LEE011 (hydrochloride)Supplier
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LEE011 (hydrochloride)(1211443-80-9)Related Product Information
- tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate
- LEE011 (succinate)
- Ribociclib
- 5-(2-Fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methyl-2,4(1H,3H)-pyrimidinedione
- 1,4-BenzenediaMine, N1-[2-(diMethylaMino)ethyl]-5-Methoxy-N1-Methyl-N4-[4-(1-Methyl-1H-indol-3-yl)-2-pyriMidinyl]-2-nitro-
- 1-(2-FLUORO-6-(TRIFLOROMETHYL)BENZYL)UREA
- Cholan-24-oic acid,6-ethyl-3-hydroxy-7-oxo-,(3α,5β,6β)-