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LEE011 succinate

Cat. No. M4889
LEE011 succinate Structure
Synonym:

Ribociclib succinate

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 100 In stock
5mg USD 80 In stock
10mg USD 100 In stock
50mg USD 250 In stock
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Quality Control
Biological Activity

CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.Responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 552.63
Formula C27H36N8O5
CAS Number 1374639-75-4
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Nature (2018). Figure 2. Ribociclib (Abmole Bioscience)
Method IB analysis
Cell Lines 4T1 tumor cell lines
Concentrations 1 μM
Incubation Time 36 h
Results "Furthermore, treatment of multiple cancer cell lines with two different selective inhibitors of CDK4/6 kinase, palbociclib or ribociclib, upregulated PD-L1 protein abundance and stability even in pRB knock-down cells."
Rating
Product Citations
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LEE011 succinate, Ribociclib succinate supplier, inhibitors

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