生物活性 体外研究 体内研究 特征 靶点
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ChemicalBook  CAS数据库列表  A66

A66

生物活性 体外研究 体内研究 特征 靶点
A66,1166227-08-2,结构式
A66
  • CAS号:1166227-08-2
  • 英文名:A66
  • 中文名:A66
  • CBNumber:CB42553771
  • 分子式:C17H23N5O2S2
  • 分子量:393.53
  • MOL File:1166227-08-2.mol
A66化学性质
  • 密度 :1.354
  • 储存条件 :Sealed in dry,Store in freezer, under -20°C
  • 溶解度 :insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming
  • 形态 :solid
  • 酸度系数(pKa) :6.27±0.70(Predicted)
  • 颜色 :Off-white to light yellow
安全信息
  • 海关编码 :29341000

A66性质、用途与生产工艺

  • 生物活性 A66是一种有效的，特异性的p110α抑制剂，IC50为32 nM，作用于p110α比作用于其他I型PI3K亚型选择性高100倍以上。
  • 体外研究 In addition to the wild-type p110α, A66 also potently inhibits the oncogenic forms of p110α such as p110α E545K and p110α H1047R with IC50 of 30 nM and 43 nM, respectively. Unlike PIK-75, A66 displays >100 fold selectivity for p110α over other class-I PI3K isoforms. Among the class-II PI3Ks, class-III PI3K and PI4Ks, A66 only exhibits limited cross-reactivity with the class-II PI3K PI3KC2β and the PI4Kβ isoform of PI4K with IC50 of 462 nM and 236 nM, respectively. A66 exhibits no inhibitory activity against other lipid kinases or the related kinases DNA-PK and mTOR. A66 has a higher degree of specificity compared with PIK-75 when tested at 10 μM against two large panels of 110 protein kinases and 318 kinases. Inhibition of p110α alone by A66 treatment is sufficient to block insulin signalling to Akt/PKB in certain cell lines that harbor H1047R mutations in PIK3CA and have high levels of p110α and class-Ia PI3K activity. A66 treatment at 0.7 μM induces a 75-80% reduction in focus formation by the highly transforming p85α iSH2 mutants KS459delN, DKRMN-S560del, and K379E, and reduces the phosphorylation of Akt on T308 by all p85 mutants.
  • 体内研究 A single dose of A66 at 100 mg/kg induces a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK, in SK-OV-3 tumour tissue in vivo at both 1 hour and 6 hours after dosing. A66 dosed at 100 mg/kg once daily (QD) for 21 days or 75 mg/kg twice daily (BID) for 16 days induces a significant delay in growth of SK-OV-3 xenografted tumors with average TGI of 45.9% and 29.9%, respectively, which is even greater than that induced by the well-established pan-PI3K inhibitor BEZ-235. QD dosing of A66 in the HCT-116 xenograft model also induces a significant reduction in tumour volume with TGI of 77.2%, but causes a non-significant reduction in tumor volume in the U87MG xenograft model. Administration of A66 at 10 mg/kg in male CD1 mice induces significant impairments in the ITT (insulin tolerance test) and GTT (glucose tolerance test), and an increase in glucose production during a PTT (pyruvate tolerance test), almost to the same level as the pan-PI3K inhibitors.
  • 特征 A66 is highly selective for p110α isoform.
  • 靶点

    p110α

    32 nM (IC 50 )

    p110α E545K

    30 nM (IC 50 )

    p110α H1047R

    43 nM (IC 50 )

    p110γ

    3480 nM (IC 50 )

    PI3K-C2β

    462 nM (IC 50 )

    PI4Kβ

    236 nM (IC 50 )

A66上下游产品信息
上游原料
下游产品
A66生产厂家
  • 公司名称：济南精合医药科技有限公司
  • 联系电话：+86 (531) 88811783
  • 电子邮件：sales@trio-pharmatech.com (International market)
  • 国家：中国
  • 产品数：1856
  • 优势度：62
  • 公司名称：China Kouting Group Limited
  • 联系电话：+86 (21) 5811-6473 5811-6475
  • 电子邮件：sales@koutingchina.com
  • 国家：中国
  • 产品数：496
  • 优势度：60
  • 公司名称：AdooQ BioScience, LLC
  • 联系电话：+1 (866) 930-6790
  • 电子邮件：info@adooq.com
  • 国家：美国
  • 产品数：2782
  • 优势度：58
  • 公司名称：上海喀露蓝科技有限公司
  • 联系电话：18149758185 18149758185
  • 电子邮件：sales-cpd@caerulumpharma.com
  • 国家：中国
  • 产品数：3466
  • 优势度：58
  • 公司名称：苏州亚科科技股份有限公司
  • 联系电话：0512-87182056 18013166090
  • 电子邮件：lingling.qi@yacoo.com.cn
  • 国家：中国
  • 产品数：7295
  • 优势度：60
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