2770108-93-3

Name	INDEX NAME NOT YET ASSIGNED
CAS	2770108-93-3
Molecular Formula	C53H61ClN8O5S
Molecular Weight	957.62
MOL File	2770108-93-3.mol

Synonyms

6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[5-[[3′-[[[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]amino]carbonyl]-5′-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4′-methyl[1,1′-biphenyl]-4-yl]oxy]pentyl]-2,3,9-trimethyl-, (6S)-

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Chemical Properties

density	1.31±0.1 g/cm3(Predicted)
form	Solid
pka	11.57±0.46(Predicted)
color	White to off-white

Hazard Information

Uses

YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer[1].

in vivo

YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells^[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice^[1].

	IP (80 mg/kg)	PO (80 mg/kg)
t_1/2 (h)	3.81	4.16
T_max (h)	1	1
C_max (ng/mL)	27126.3	4383.6
AUC_0-24 (ng/mL·h)	273220.1	13509.1
CL (mL/min/kg)	4.88
F (%)		4.94

Animal Model:	BALB/c nude mice (injected with A549 or AsPC-1)^[1]
Dosage:	60 mg/kg
Administration:	IP; every other day, for 38 days
Result:	Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.

IC 50

EZH2; EZH2: 490 nM (IC₅₀); BRD4: 34 nM (IC₅₀)

References

[1] Guo Z, et al. Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors. J Med Chem. 2022;65(9):6573-6592. DOI:10.1021/acs.jmedchem.1c01876

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