R-8200 Ribociclib, Free Base, >99%

Synonyms : [Lee011]

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  • 5 mg
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  • 40
  • 35
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  • 10 mg
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  • 56
  • 48
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  • 25 mg
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  • 82
  • 71
  • 9,900
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  • 50 mg
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  • 104
  • 90
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  • 100 mg
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  • 169
  • 145
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  • 200 mg
  • 299
  • 277
  • 239
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  • 250 mg
  • 359
  • 333
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  • 500 mg
  • 522
  • 484
  • 418
  • 58,100
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  • 1 g
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  • 896
  • 772
  • 107,500
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  • M.W. 434.54
  • C23H30N8O
  • [1211441-98-3]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO.

  • Ribociclib, also known as LEE011, is a highly specific CDK4/6 inhibitor. It significantly inhibited proliferation in 12 of 17 human neuroblastoma-derived cell lines with an average IC50 value of 307 nM in the 12 sensitive cell lines. It also caused cell-cycle arrest and cellular senescence that might be related to decreases in phosphorylated RB and FOXM1, respectively. In addition, ribociclib induced subcutaneous neuroblastoma xenograft growth delay in vivo. Rader J. et al. "Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma." Clin. Cancer Res. 19: 6173-6182 (2013).
  • Ribociclib inhibited CDK4/6 kinase activity with IC50 value at the nM level and showed high selectivity for these targets. In a number of preclinical tumor models, ribociclib demonstrated anti-tumor activity that correlated with CDK4/6 inhibition. Ribociclib showed anti-tumor activity in melanoma and breast cancer models as a single agent or in combination with other agents. Kim S. et al. "LEE011: An orally bioavailable, selective small molecule inhibitor of CDK4/6– Reactivating Rb in cancer." Mol. Cancer Ther. 12: Abstract PR02 (2013).
  • A Phase 1 study of ribociclib demonstrated an acceptable safety profile, dose dependent PK, and preliminary clinical activity in patients with advanced solid tumors or lymphomas. Infante J.R. et al. "Phase 1 multicenter, open label, dose-escalation study of LEE011, an oral inhibitor of cyclin-dependent kinase 4/6, in patients with advanced solid tumors or lymphomas." Mol. Cancer Ther. 12: Abstract A276 (2013).
  • Related CAS numbers: 1211443-80-9 for the hydrochloride salt; 1374639-75-4 for the succinate (1:1) salt; 1374639-79-8 for the (1:1) succinate hydrate salt, whose hydration level was not specified.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
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