LEE011 (succinate)
LEE011 (succinate) Basic information
- Product Name:
- LEE011 (succinate)
- Synonyms:
-
- LEE011 (succinate)
- 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate
- LEE-011 succinate salt, Ribociclib succinate salt
- Ribociclib succinate
- Ribociclib Succinate (Kisqali)
- RIBOCICLIB SUCCINATE (LEE011 SUCCINATE)
- Ribociclib succite
- RIBOCICLIB SUCCINATE (LEE011)
- CAS:
- 1374639-75-4
- MF:
- C27H36N8O5
- MW:
- 552.64
- Product Categories:
-
- API
- Mol File:
- 1374639-75-4.mol
LEE011 (succinate) Chemical Properties
- Melting point:
- >160oC (dec.)
- storage temp.
- Refrigerator
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- color
- Pale Beige
- InChIKey
- NHANOMFABJQAAH-UHFFFAOYSA-N
- SMILES
- C(C(=O)O)CC(=O)O.C(C1=CC2=CN=C(NC3N=CC(N4CCNCC4)=CC=3)N=C2N1C1CCCC1)(=O)N(C)C
LEE011 (succinate) Usage And Synthesis
Uses
LEE011 is an orally bioavailable and highly specific CDK4/6 (cyclin-dependent kinase 4/6) inhibitor. LEE011 in combination with LGX818 (a V600E BRAF specific inhibitor) or BYL719 (a PIK3CA specific inhibitor) leads to robust anti-tumor activity in melanoma and breast cancer tumor models.
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)
LEE011 (succinate)Supplier
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- 021-61350663 15502154572
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- 13621628489
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- 13970866816
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- 0755-23284190 13421666688
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- 15169181595
- ming.zhang3@portonpharma.com
LEE011 (succinate)(1374639-75-4)Related Product Information
- tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate
- LEE011 (hydrochloride)
- Ribociclib
- Neratinib Maleate
- 1-Piperazinecarboxylic acid, 4-[6-[[7-cyclopentyl-6-[(diMethylaMino)carbonyl]-7H-pyrrolo[2,3-d]pyriMidin-2-yl]aMino]-3-pyridinyl]-, 1,1-diMethylethyl ester
- 2-Chloro-7-cyclopentyl-N,N-dimethyl-H-pyrrolo[2,3-d]pyrimidine-6-carboxamide