AS-99 TFA (C09-1103-407)

AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor ( IC 50 = 0.79 µM, K d = 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusiAppearance:SolidIC50& Target:0.79 µM (ASH1L histone methyltransferase)In Vitro:AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 µM of AS-99 TFA on any of the tested histone methyltransferases, indicating over 100-fold selectivityIn Vivo:AS-99 (30mg/kg; i.p.; q.d., treated for 14 consecutive days) TFA reduces leukemia burden in mice. AS-99 TFA is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 1Biological Activity:AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor ( IC 50 =u20090.79u2009µM, K d =u20090.89u2009µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downre. Specification: 0.99 Molecular Formula: C29H31F6N5O5S2 Molecular Weight: 707.71