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CPI-360

Cat. No. M5186
CPI-360 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 300 In stock
50mg USD 960 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM. CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM respectively in KARPAS-422 cells. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis. CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44% in mice bearing KARPAS-422 xenografts.

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 437.53
Formula C25H31N3O4
CAS Number 1802175-06-9
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.
Bradley WD, et al. Chem Biol. 2014 Nov 20;21(11):1463-75. PMID: 25457180.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CPI-360 supplier, Histone Methyltransferase, inhibitors

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