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CPI-169

Item № 18299
CAS № 1450655-76-1
Purity ≥98%
product image
                (CAS 1450655-76-1)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $55.00 0.00
     5 mg $193.00 0.00

Pricing updated 2019-04-24. Prices are subject to change without notice.

Description

The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. CPI-169 is a selective EZH2 inhibitor with IC50 values of 0.24, 0.51, and 6.1 nM for wild-type EZH2, Y641N mutant EZH2, and wild-type EZH1, respectively.1 It decreases cellular levels of H3K27me3 (EC50 = 70 nM), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines.1 With subcutaneous administration of 200 mg/kg/twice a day, CPI-169 was shown to inhibit tumor growth in a NHL xenograft model, reducing global H3K27me3.1 It has also been shown to synergize with the B-cell lymphoma 2 inhibitor, ABT-199 (Item No. 16233), to suppress the growth of NHL cell lines.1

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Technical Information
Formal Name
N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-1H-indole-3-carboxamide
CAS Number
1450655-76-1
Molecular Formula
C27H36N4O5S
Formula Weight
528.7
Purity
≥98%
Formulation
A crystalline solid
λmax
291 nm
SMILES
CC(NC1=O)=CC(OC)=C1CNC(C2=C(C)N(C(C)C3CCN(S(CC)(=O)=O)CC3)C4=C2C=CC=C4)=O
InChI Code
InChI=1S/C27H36N4O5S/c1-6-37(34,35)30-13-11-20(12-14-30)18(3)31-19(4)25(21-9-7-8-10-23(21)31)27(33)28-16-22-24(36-5)15-17(2)29-26(22)32/h7-10,15,18,20H,6,11-14,16H2,1-5H3,(H,28,33)(H,29,32)
InChI Key
LHGUZCKPFXXVPV-UHFFFAOYSA-N

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

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

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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References & Product Citations
Product Description References

1. Bradley, W.D., Arora, S., Busby, J., et al. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation Chemistry & Biology 21, 1-13 (2014).

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