产品名称

英文名称：PIK-75

同义词

PIK-75 Hydrochloride、372196-77-5、PIK-75 HCl、(E)-N'-((6-bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride、1462995-14-7、PIK75hydrochloride、7GH4IC9PLL、PIK-75 (hydrochloride)、N-[(E)-(6-bromoimidazo[1,2-a]pyri

产品性质

CAS编号：372196-77-5

分子式：C16H14BrN5O4S·HCl

分子量：488.74

PubChem编号：45265864

英文别名：PIK-75 Hydrochloride|372196-77-5|PIK-75 HCl|(E)-N'-((6-bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride|1462995-14-7|PIK75hydrochloride|7GH4IC9PLL|PIK-75 (hydrochloride)|N-[(E)-(6-bromoimidazo[1,2-a]pyri

规格或纯度：≥98%

英文名称：PIK-75

生化机理：PIK-75 Hydrochloride is a hydrochloride salt form of PIK-75, which is a preferential p110α/γ forms of PI3K inhibitor with IC50 of 6, 1300, 76, 510 nM for p110α, p110β, p110γ, p110δ, respectively. PIK-75 is a PI3K p110α specific inhibitor and belongs to the class of imidazo[1, 2-a]pyridines. It inhibited cell proliferation of A375 cells (IC50=58nM) in vitro and reduced tumor growth in a mouse xenograft model. Besides inhibition of PI3Kα, PIK-75 also inhibited DNA-PK with an IC50 of 2 nM, but not mTORC1 and mTORC2. PIK-75-mediated anti-inflammatory effects are associated with dramatic inhibition of AKT phosphorylation, IKK activation and NF-κB transcription.Selective inhibitor of p110α (IC 50 values are 5.8, 76 nM and 1.3 μM at p110α, p110γ and p110β, respectively). Inhibits production of PIP 2 and PIP 3 in adipocytes, phosphorylation of Akt and activation of mTORC1. Cell-permeable.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：PIK-75是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，亚型特异性的突变体在Ser773，也有效抑制DNA-PK，IC50为2 nM。PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.

IUPAC Name：N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide;hydrochloride

INCHI：InChI=1S/C16H14BrN5O4S.ClH/c1-11-3-5-13(22(23)24)7-15(11)27(25,26)20(2)19-9-14-8-18-16-6-4-12(17)10-21(14)16;/h3-10H,1-2H3;1H/b19-9+;

InChi Key：VOUDEIAYNKZQKM-MYHMWQFYSA-N

Canonical SMILES：CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)N=CC2=CN=C3N2C=C(C=C3)Br.Cl

Isomeric SMILES：CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br.Cl

PubChem CID：45265864

溶解性：DMSO ≥16mg/mL Water <1.2mg/mL Ethanol ≥4.6mg/mL

产品包装