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Tazemetostat hydrobromide

Cat. No. M10532
Tazemetostat hydrobromide Structure
Synonym:

EPZ-6438 hydrobromide; Tazemetostat HBr

Size Price Availability
10mg USD 80  USD80 4-7 Days
25mg USD 110  USD110 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Tazemetostat (EPZ-6438) hydrobromide is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM. 

In vivo, Tazemetostat (250 or 500 mg/kg; twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors.

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 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.

Chemical Information
Molecular Weight 653.65
Formula C34H45BrN4O4
CAS Number 1467052-75-0
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

[1] Sarah K Knutson, et al. Proc Natl Acad Sci U S A. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

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Keywords: Tazemetostat hydrobromide, EPZ-6438 hydrobromide; Tazemetostat HBr supplier, Histone Methyltransferase, inhibitors

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