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
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AS-99 TFA
CAS number：unknown molecular formula：C29H31F6N5O5S2
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| Chinese alias | AS-99 三氟乙酸 | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C29H31F6N5O5S2 |
| molecular weight | 707.71 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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