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EPZ020411

Item № 19160
CAS № 1700663-41-7
Purity ≥98%
product image
                (CAS 1700663-41-7)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $37.00 0.00
     5 mg $167.00 0.00
     10 mg $296.00 0.00
     25 mg $648.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).1 It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM).1 EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.1

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Technical Information
Formal Name
N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine
CAS Number
1700663-41-7
Molecular Formula
C25H38N4O3
Formula Weight
442.6
Purity
≥98%
Formulation
A crystalline solid
λmax
250 nm
SMILES
CN(CCNC)CC1=CNN=C1C(C=C2)=CC=C2O[C@H](C3)C[C@@H]3OCCC4CCOCC4
InChI Code
InChI=1S/C25H38N4O3/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28)/t23-,24-
InChI Key
QMDKVNSQXPVCRD-RQNOJGIXSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Mitchell, L.H., Drew, A.E., Ribich, S.A., et al. Aryl pyrazoles as potent inhibitors of arginine methyltransferases: Identification of the first PRMT6 tool compound ACS Med. Chem. Lett. 6, 655-659 (2015).

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