SML2520

MI-503

≥98% (HPLC)

• 동의어(들): 1-((1H-Pyrazol-4-yl)methyl)-4-methyl-5-((4-(6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile, 4-Methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indole-2-carbonitrile, MI 503, MI503
• 실험식(Hill 표기법): C₂₈H₂₇F₃N₈S
• CAS Number: 1857417-13-0
• Molecular Weight: 564.63
• MDL number: MFCD28506303
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• 양식: powder
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear
• 저장 온도: −20°C
• SMILES string: FC(F)(F)Cc1[s]c2ncnc(c2c1)NC3CCN(CC3)Cc4c(c5c([n](c(c5)C#N)Cc6c[nH]nc6)cc4)C
• InChI key: DETOMBLLEOZTMZ-UHFFFAOYSA-N

설명

생화학적/생리학적 작용

Highly potent menin-MLL interaction inhibitor that selectively inhibits MLL oncogenic fusions-driven cancer progression in vitro and in vivo.

MI-503 is a highly potent menin-MLL interaction inhibitor (cell-free IC50 = 14.7 nM against 1 nM FITC-MLL(4-13) peptide; cellular IC50 = 220 nM using HEK293 MLL-AF9 fusion transfectants) that targets menin MLL-binding site with high affinity (KD = 9.3 nM by ITC). MI-503 selectively inhibits mixed lineage leukemia (MLL) oncogenic fusion-driven cancer progression in cultures (GI50 from 250 to 570 nM; GI50 >5 μM against cells without MLL gene translocation) and is efficacious against human MLL leukemia MV4;11 tumor growth in mice in vivo (by 80-100%; 60 mg/kg/day i.p.) with good pharmacokinetic properties, oral bioavailability (73% post 30 mg/kg p.o.), and no adverse effects to the animals.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable