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Ribociclib succinate (LEE011 succinate)

Cat. No. M4889
Ribociclib succinate (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 67  USD67 In stock
2mg USD 40  USD40 In stock
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 120  USD120 In stock
100mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Ribociclib succinate (LEE011 succinate) is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. 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.

Product Citations
Customer Product Validations & Biological Datas
Source Nature (2018). Figure 2. Ribociclib
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."
Chemical Information
Molecular Weight 552.63
Formula C27H36N8O5
CAS Number 1374639-75-4
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

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  Catalog
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