AS-99 TFA

AS-99 三氟乙酸

AS-99 TFA

A659364-5mg

5mg

≥99%

2-8°C储存,干燥

冰袋运输

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 fusi Appearance:Solid IC50& 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 selectivity In 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 1 Biological 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

C29H31F6N5O5S2

707.71 g/mol

O=C(C1CN(C)C1)NCC2=CC3=C(C=C2)C(C4=CC=CC(C(N)=S)=C4)=CN3C5CCN(S(=O)(C(F)(F)F)=O)CC5.O=C(O)C(F)(F)F

DMSO : 100 mg/mL (141.30 mM; Need ultrasonic) H2O : 12.5 mg/mL (17.66 mM; Need ultrasonic)