产品名称

英文名称：PIK-90

同义词

PIK-90、677338-12-4、PIK90、N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)nicotinamide、PIK 90、CID 6857685、N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide、N-(7,8-Dimethoxy-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl)

产品性质

CAS编号：677338-12-4

分子式：C18H17N5O3

分子量：351.36

PubChem编号：135398491

英文别名：PIK-90|677338-12-4|PIK90|N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)nicotinamide|PIK 90|CID 6857685|N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide|N-(7,8-Dimethoxy-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl)

规格或纯度：98%

英文名称：PIK-90

生化机理：PIK-90 is a PI3K inhibitor,IC50=11, 350, 18, and 58 for p110 α, β, γ and δ isoforms.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：PIK-90是一种广谱的PI3K抑制剂，对p110α、p110β、p110γ和p110δ的IC50值分别为11 nM、350 nM、18 nM和58 nM。 研究表明，PIK-90在1 μmol/L时可诱导IgE分泌水平增加，但在2 μmol/L以上剂量时则可抑制IgE生成[2]。PIk-90可阻断Akt磷酸化。在LN229 PTENWT细胞中，PIK-90与CDK2抑制剂联合使用可诱发细胞凋亡。此外，PIK-90与CDK1和CDK2的siRNA联合使用可诱发细胞死亡，但是PIK-90与CDK1或CDK2的siRNA联合使用则无细胞凋亡效果。 在植入GBM43细胞的裸鼠中，PIK-90与roscovitine联合使用可显著减少肿瘤大小。 PIK-90是一种PI3Kα/γ/δ抑制剂，IC50分别为11 nM/18 nM/58 nM，对PI3Kβ作用效果稍弱。A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).

PubChem SID：488202817

IUPAC Name：N-(7,8-dimethoxy-2,3-dihydro-1H-imidazo[1,2-c]quinazolin-5-ylidene)pyridine-3-carboxamide

INCHI：InChI=1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10,20H,8-9H2,1-2H3

InChi Key：FCKJZIRDZMVDEM-UHFFFAOYSA-N

Canonical SMILES：COC1=C(C2=NC(=NC(=O)C3=CN=CC=C3)N4CCNC4=C2C=C1)OC

Isomeric SMILES：COC1=C(C2=NC(=NC(=O)C3=CN=CC=C3)N4CCNC4=C2C=C1)OC

PubChem CID：135398491

溶解性：DMSO 0.28 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

敏感性：对光线敏感

产品包装