1. PI3K/Akt/mTOR
    Anti-infection
  2. Akt
    Parasite
  3. Miransertib

Miransertib (Synonyms: ARQ-092)

製品番号: HY-19719 純度: 99.77%
取扱説明書

Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Miransertib 構造式

Miransertib 構造式

CAS 番号 : 1313881-70-7

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 137 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 96 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 252 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1092 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2040 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Akt アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research[1]. Miransertib is effective against Leishmania[2].

IC50 & Target[1][2]

Akt1

2.7 nM (IC50)

Akt3

8.1 nM (IC50)

Akt2

14 nM (IC50)

Akt1 E17K mutant

 

Leishmania

 

体外実験

In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31 μM)[1].
Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages[2]

体内実験

Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf was 5496 h•ng/mL and 2960 h•ng/mL in rats and monkeys, respectively[1].
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma[1].

臨床実験
分子量

432.52

分子式

C₂₇H₂₄N₆

CAS 番号

1313881-70-7

SMILES

NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 12.5 mg/mL (28.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3120 mL 11.5602 mL 23.1203 mL
5 mM 0.4624 mL 2.3120 mL 4.6241 mL
10 mM 0.2312 mL 1.1560 mL 2.3120 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[1]

Anti-proliferative cellular assays are conducted using the CellTiter Non-Radioactive Cell Proliferation Assay, which utilizes the production of formazan from a tetrazolium compound by live cells. AN3CA and A2780 cells are obtained from the ATCC. AN3CA cells are cultured in DMEM, and A2780 cells are cultured in RPMI. Cells are plated in 96-well plates at 2,000-10,000 cells/well, cultured for 24 h, and treated with the test compound for 72 h at a final DMSO concentration no greater than 0.5% v/v. PMS stock reagent (0.92 mg/mL in DPBS) is diluted 20-fold in MTS stock reagent (2 mg/mL in DPBS), and this MTS/PMS mixture is diluted 5-fold into each well of the 96-well plate. The plates are incubated for 3-4 h, and the absorbance of formazan is measured at 490 nm. The data are normalized to the untreated controls, the dose-response curves are fit to a four-parameter logistic equation, and the IC50 values are determined. All IC50 values reported are the geometric mean of at least two independent determinations[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

Mice[2]
SHP2Y279C/+ mice are used. Only male progeny are used for the experiments herein and all mice are maintained on outbred C57BL6/J backgrounds, backcrossed for more than 10 generations. Either vehicle or Miransertib (100 mg/kg body weight) is then daily administered by oral gavage for 4 weeks. Administration began at 12 weeks of age (after established hypertrophy is indicated), and continued for 4 weeks, until the mice reach 16 weeks of age. As controls, SHP2+/+ and SHP2Y279C/+ mice are treated with vehicle alone.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • モル濃度カルキュレーター

  • 希釈カルキュレーター

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MiransertibARQ-092ARQ092ARQ 092AktParasitePKBProtein kinase BAkt1Akt2Akt3AKT1-E17Kanti-tumoranti-proliferativep-Aktp-PRAS40Inhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

 

タイトル

お名前 *

 

PC 用メールアドレス *

電話番号 *

 

勤務先/学校名 *

Department *

 

カスタマ需要量 *

国会或いは地域 *

     

必ず会社名を記載ください。個人への返信は行いません。

メッセージ

バルクお問い合わせ

Inquiry Information

製品名:
Miransertib
製品番号:
HY-19719
数量:
MCE 日本正規代理店: