SML2942
LY2857785 free base
≥98% (HPLC)
别名:
LY 2857785 free base, LY-2857785 free base, N1-[4-(3-isopropyl-2-methyl-indazol-5-yl) pyrimidin-2-yl]-N4-tetrahydropyran-4-yl-cyclohexane-trans-1, 4-diamine
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关于此项目
经验公式（希尔记法）:
C26H36N6O
化学文摘社编号:
分子量:
448.60
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
CN1C(C(C)C)=C2C(C=CC(C3=NC(N[C@H]4CC[C@H](NC5CCOCC5)CC4)=NC=C3)=C2)=N1
InChI
1S/C26H36N6O/c1-17(2)25-22-16-18(4-9-24(22)31-32(25)3)23-10-13-27-26(30-23)29-20-7-5-19(6-8-20)28-21-11-14-33-15-12-21/h4,9-10,13,16-17,19-21,28H,5-8,11-12,14-15H2,1-3H3,(H,27,29,30)/t19-,20-
InChI key
LHIUZPIDLZYPRL-MXVIHJGJSA-N
Biochem/physiol Actions
ATP-competitive, potent and reversible CDK9/4/8, DYRK2, FLT3-D835Y inhibitor with anticancer efficacy in vitro and in vivo.
LY2857785 is an ATP-competitive, potent and reversible CDK9/4/8 (IC50 =11 nM/CDK9-CycT, 12 nM/CDK4-CycD1, 16 nM/CDK8-CycC), DYRK2 (IC50 = 44 nM) and FLT3-D835Y (IC50 = 23 nM) inhibitor that significantly reduces cellular RNAP II CTD phosphorylation (U2OS pSer2/pSer5 IC50 =89/42 nM) with good selectivity over a panel of 109 kinase constructs (IC50 = 0.1-1μM/wt FLT3, CDK1/2/3/5/7, PIM1/2; >1 μM/100 kinases). LY2857785 exhibits antiproliferation efficacy in a wide-range cancer cultures (IC50 ∼30 nM-1 μM), and causes AML MV-4-11 xenograft tumor regression in rats (3-9 mg/kg, i.v. infusion Q5Dx5) and mice (8-10 mg/kg, i.v. bolus Q3Dx5) in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
null
Tinggui Yin et al.
Molecular cancer therapeutics, 13(6), 1442-1456 (2014-04-02)
DNA-dependent RNA polymerase II (RNAP II) largest subunit RPB1 C-terminal domain (CTD) kinases, including CDK9, are serine/threonine kinases known to regulate transcriptional initiation and elongation by phosphorylating Ser 2, 5, and 7 residues on CTD. Given the reported dysregulation of
Qi Xie et al.
The Journal of clinical investigation, 126(7), 2757-2772 (2016-06-21)
Glioblastomas co-opt stem cell regulatory pathways to maintain brain tumor-initiating cells (BTICs), also known as cancer stem cells. NOTCH signaling has been a molecular target in BTICs, but NOTCH antagonists have demonstrated limited efficacy in clinical trials. Recombining binding protein
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML2942-5MG | 04061841877332 |
| SML2942-25MG | 04061841877301 |