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EPZ015666

Cat. No. M4954
EPZ015666 Structure
Synonym:

GSK3235025

Size Price Availability Quantity
10mM*1mL in DMSO USD 90  USD90 In stock
2mg USD 55  USD55 In stock
5mg USD 85  USD85 In stock
10mg USD 140  USD140 In stock
25mg USD 285  USD285 In stock
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Quality Control & Documentation
Biological Activity

EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models.

Chemical Information
Molecular Weight 383.44
Formula C20H25N5O3
CAS Number 1616391-65-1
Solubility (25°C) DMSO 60 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.

References

[1] Xing Liu, et al. EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma

[2] Changhui Diao, et al. Inhibition of PRMT5 Attenuates Oxidative Stress-Induced Pyroptosis via Activation of the Nrf2/HO-1 Signal Pathway in a Mouse Model of Renal Ischemia-Reperfusion Injury

[3] Guozhen Gao, et al. PRMT1 loss sensitizes cells to PRMT5 inhibition

[4] Gregory V Kryukov, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells

[5] Elayne Chan-Penebre, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

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  Catalog
Abmole Inhibitor Catalog




Keywords: EPZ015666, GSK3235025 supplier, PRMTs, inhibitors, activators


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