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PF-AKT400

COA COA
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
P650945-5mg
 5mg 期货 Stock Image
P650945-10mg
 10mg 期货 Stock Image
P650945-50mg
 50mg 期货 Stock Image
P650945-100mg
 100mg 期货 Stock Image
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Akt (179) PI3K/Akt/mTOR (764)
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基本描述

规格或纯度 ≥98%
英文名称 PF-AKT400
生化机理 PF-AKT400 是一种具有广泛选择性的强效 ATP 竞争性 Akt 抑制剂，对 PKBα 的选择性（IC 50 =0.5 nM）比对 PKA 的选择性（IC 50 =450 nM）高出 900 倍。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα ( IC 50 =0.5 nM) than PKA ( IC 50 =450 nM).

In Vitro

PF-AKT400 (Compound 42) provides significantly enhanced selectivity for Akt relative to earlier leads such as spiroindoline 2. Free IC 50 and EC 50 values are estimated for phospho-S6 reduction (110 nM) and Akt hyperphosphorylation (216 nM), respectively. These values corresponded well to the cellular IC 50 for PF-AKT400 in U87 cells measuring p-GSK-3α (310 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-AKT400 is subsequently evaluated for modulation of Akt in tumors and in multiple in vivo mouse models of antitumor efficacy. It is active in a PC3 prostate carcinoma xenograft experiment, with 75% TGI observed at 100 mg/kg b.i.d. dosing for 10 days. In a colorectal carcinoma (Colo205) xenograft study, PF-AKT400 produces 60% TGI at 150 mg/kg b.i.d. after 10 days. Most intriguingly, in combination with Rapamycin (10 mg/kg, ip), 75 mg/kg b.i.d. (10 days) of PF-AKT400 results in 98% TGI in an additional PC3 prostate carcinoma xenograft study compared to 56% TGI and 66% TGI with PF-AKT400 and Rapamycin as single agents. To define the in vivo potency of PF-AKT400 (Compound 42) in the PC3 xenograft model, oral administration of 25, 75, and 100 mg/kg PF-AKT400 is performed with blood and tumor sampling over time. Immunoblot analysis of detergent-soluble extracts derived from PC3 tumors shows a significant reduction of S6 phosphorylation, and hyperphosphorylation of Akt upon treatment at doses that produced significant tumor growth inhibition. Plasma drug concentrations peak rapidly after oral administration of doses between 25-100 mg/kg (T max =0.5 h). Peak PD responses of phospho-S6 and phospho-Akt are observed at approximately 2-4h and 1h post-administration of PF-AKT400, respectively. The time-course of PD marker response is well described by a PK/PD model at doses that ranged from no efficacy (25 mg/kg) to maximal efficacy (100 mg/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal administration

Mice Studies to describe the PK/PD relationship for PF-AKT400 are performed in male SCID/Beige mice bearing subcutaneous PC3 prostate carcinoma xenografts. Once tumors reach about ~300mm 3 in size, PF-AKT400 is formulated in 0.5% methylcellulose vehicle and administered orally to 3 mice per dose group. Plasma and tumors are harvested over time, tumor lysates prepared, and the levels of phospho S6 reduction and phospho Akt induction are evaluated by immunoblot. aladdin has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:PKBα 0.5 nM (IC 50 ) PKA 450 nM (IC 50 )
纯度 ≥98%

关联靶点（人）

AKT3 Tchem RAC-γ 丝氨酸/苏氨酸蛋白激酶(RAC-gamma serine/threonine-protein kinase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AKT2 Tchem RAC-β丝氨酸/苏氨酸蛋白激酶(RAC-beta serine/threonine-protein kinase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AKT1 Tchem RAC-alpha 丝氨酸/苏氨酸蛋白激酶(RAC-alpha serine/threonine-protein kinase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKG1 Tchem cGMP-dependent protein kinase 1 beta (2814 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha 2 (2184 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT1 Tchem Serine/threonine-protein kinase AKT (9192 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA3 Tchem Ribosomal protein S6 kinase alpha 3 (4284 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CDK7 Tchem Cyclin-dependent kinase 7 (1512 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
COLO 205 (50209 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver microsomes (16955 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Canis familiaris (36305 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name N-[[(3S)-3-amino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl]-2,4-difluorobenzamide
INCHI 1S/C20H22F2N6O/c1-2-12-8-24-17-16(12)18(27-11-26-17)28-6-5-20(23,10-28)9-25-19(29)14-4-3-13(21)7-15(14)22/h3-4,7-8,11H,2,5-6,9-10,23H2,1H3,(H,25,29)(H,24,26,27)/t20-/m0/s1
InChi Key MOZRQQTUYAYCQT-FQEVSTJZSA-N
Smiles CCC1=CNC2=C1C(=NC=N2)N3CCC(C3)(CNC(=O)C4=C(C=C(C=C4)F)F)N
Isomeric SMILES CCC1=CNC2=C1C(=NC=N2)N3CC[C@@](C3)(CNC(=O)C4=C(C=C(C=C4)F)F)N
PubChem CID 25061501
分子量 400.43

化学和物理性质

溶解性 DMSO : ≥ 100 mg/mL (249.73 mM)
分子量 400.400 g/mol
XLogP3 2.200
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 7
可旋转键计数Rotatable Bond Count 5
精确质量Exact Mass 400.182 Da
单同位素质量Monoisotopic Mass 400.182 Da
拓扑极表面积Topological Polar Surface Area 99.900 Ų
重原子数Heavy Atom Count 29
形式电荷Formal Charge 0
复杂度Complexity 597.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 1
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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