ChemicalBook CAS DataBase List 2225938-86-1

2225938-86-1

Name	1H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[6-[4-[2-[[3-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]-1-oxopropyl]amino]ethyl]-1-piperazinyl]-3-pyridinyl]-1-(1-methylethyl)-
CAS	2225938-86-1
Molecular Formula	C48H55N11O8
Molecular Weight	914.02
MOL File	2225938-86-1.mol

Chemical Properties

Boiling point	1203.6±65.0 °C(Predicted)
density	1.44±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 2mg/mL, clear (Warmed)
form	Solid
pka	10.74±0.40(Predicted)
color	Light yellow to yellow

Hazard Information

Description

MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.

Uses

in vivo

MS177 (100?mg/kg, i.p., BID for 6 days) represses tumor growth in PDX animal model of MLL-r AML, and in subcutaneously xenografted MLL-r leukaemia models^[1].
MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice^[1].
MS177 (100?mg/kg, i.p., BID for 6?days per week; and 200?mg/?kg, i.p. BID 3?days per week) is well tolerated and lacks apparent toxicity in mice^[1].

Animal Model:	PDX animal model of MLL-r AML^[1]
Dosage:	100?mg/kg
Administration:	Intraperitoneal injection (i.p.), BID for 6 days.
Result:	Inhibited tumor growth and prolonged survival.

IC 50

EZH2

storage

Store at -20°C

References

[1] Wang J, et al. EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis. Nat Cell Biol. 2022 Mar;24(3):384-399. DOI:10.1038/s41556-022-00850-x

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