Ribociclib succinate
CAS No. 1374639-75-4
Ribociclib succinate ( LEE011 succinate )
Catalog No. M22128 CAS No. 1374639-75-4
Ribociclib succinate is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
2MG | 27 | In Stock |
|
5MG | 42 | In Stock |
|
10MG | 60 | In Stock |
|
25MG | 88 | In Stock |
|
50MG | 105 | In Stock |
|
100MG | 159 | In Stock |
|
200MG | 257 | In Stock |
|
500MG | 458 | In Stock |
|
1G | Get Quote | In Stock |
|
Biological Information
-
Product NameRibociclib succinate
-
NoteResearch use only, not for human use.
-
Brief DescriptionRibociclib succinate is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
-
DescriptionRibociclib succinate is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex. Ribociclib succinate treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition causes a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively. Treatment with Ribociclib obviously inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Treating a panel of 17 neuroblastoma cell lines with Ribociclib across a four-log dose range (10 to 10,000 nM) .Tumor growth is obviously delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment. 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 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.
-
SynonymsLEE011 succinate
-
PathwayAngiogenesis
-
TargetCDK
-
RecptorCDK4;CDK6
-
Research AreaCancer
-
IndicationAdvanced Breast Cancer
Chemical Information
-
CAS Number1374639-75-4
-
Formula Weight552.63
-
Molecular FormulaC27H36N8O5
-
Purity>98% (HPLC)
-
SolubilityDMSO:41 mg/mL (74.19 mM; Need ultrasonic)
-
SMILESOC(=O)CCC(O)=O.CN(C)C(=O)c1cc2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n1C1CCCC1
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
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.
molnova catalog
related products
-
ML365
ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).
-
Senexin B
Senexin B (SNX2-1-165) is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 of 24-50 nM.
-
TCS 1102
TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2/3 nM for OX2/1 receptors).