PHT-427 化学構造
分子量: 409.61



Quality Control & MSDS


  • Compare Akt Inhibitors
  • 研究分野
  • Combination Therapy



情報 PHT-427は、二重AktとPDPK1阻害剤で、Ki が それぞれ2.7 μM と 5.2 μMです。
目標 Akt PDPK1
IC50 2.7 μM 5.2 μM [1]
In vitro試験 PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. [1] PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells with IC50 of 65 μM. [2]
In vivo試験 PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg. [1]

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

Surface plasmon resonance (SPR) spectroscopy binding assays All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less.

細胞アッセイ: [2]

細胞系 Panc-1 cells
濃度 1-50 μM
方法 Cell growth inhibition is determined using a micro-cytoxicity assay. Cells are plated in 96-well micro-cytoxicity at 5-10 × 103 cells per well (depending on cell doubling time) and grown for 7 days. PHT-427 dissolved in DMSO is added directly to the media, at various concentrations ranging from 1 to 50 μM. The endpoint is spectrophotometric determination of the protein content of each well using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. A concentration-response relationship at two or more concentration levels is used to obtain an IC50 for PHT-427.

動物実験: [1]

動物モデル BxPC-3, Panc-1, MiaPaCa-2, PC-3, SKOV-3, A-549 or MCF-7 cells are injected subcutaneously into the flanks of female scid mice.
製剤 40 to 50 mg/mL in sesame seed oil
投薬量 125-250 mg/kg
管理 Oral administration
Solubility 5% DMSO/95% Corn oil 5 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download PHT-427 SDF
分子量 409.61


CAS No. 1191951-57-1
保管 2年-20℃
6月-80℃in DMSO
別名 CS-0223
溶解度 (25°C) * In vitro DMSO 82 mg/mL (200.19 mM)
<1 mg/mL (<1 mM)
エタノール 60 mg/mL (146.48 mM)
In vivo 5% DMSO/95% Corn oil 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide


カスタマーレビュー (1)

Click to enlarge
Source Blood, 2011, 118, 2840-2848. PHT-427 purchased from Selleck
Method Luciferase reporter assays
Cell Lines 32D cells, BCR-ABL cells
Concentrations 20 μM
Incubation Time 24 h
Results Treatment of 32D/BCR-ABL cells withthe AKT/PDPK1 inhibitor PHT-427, the PI3K inhibitor LY294002 or the BCR-ABL inhibitor imatinib substantially reduced Atf5 promoter-directed luciferase activity.

製品表彰状 (2)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related Akt 阻害剤

  • AT13148

    AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

  • VE-822

    VE-822 is a selective ATR inhibitor with Ki of < 0.2 nM, >170-fold ATR-selectivity over the closely related PI3K-related kinases ATM/DNA-PK.

    Features:VE-822 is a highly selective and potent derivative of the ATR inhibitor VE-821.

  • WZ4003

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases.

  • AZ20

    AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR.

    Features:AZ20 is the first reported inhibitor of ATR protein kinase demonstrating tumor growth inhibition in vivo.

  • MK-2206 2HCl

    MK-2206 2HClは高度選択的に Akt1, Akt2 and Akt3を抑制して、 IC50がそれぞれ 8 nM, 12 nM と 65 nMになる。

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • AZD5363

    AZD5363は、有力なAkt阻害剤で、Akt1、Akt2とAkt3に作用すると、 IC50がそれぞれ 3 nM、 8 nM 、 8 nMです。

    Features:Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.

  • Ipatasertib (GDC-0068)

    Ipatasertib (GDC-0068)は、5nM、18nMと8nMのIC50でAkt1、Akt2とAkt3を目標としている非常に選択的な汎Akt阻害剤です。

  • Perifosine (KRX-0401)

    Perifosine (KRX-0401)は、4.7 nMのIC50による新しいAkt阻害剤です。

  • GSK690693

    GSK690693は、Akt1、Akt2とAkt3を目標としている汎Akt阻害剤で、IC50 がそれぞれ 2 nM、13 nM、9 nMです。

  • A-674563

    A-674563は、Akt1 抑制影響を示しまして、Ki が 11 nMです。

    Features:Orally bioavailable compound (achieved by replacing indole of A-443654 with phenyl moiety) and somewhat less selective for Akt over PKA than A-443654.


Tags: PHT-427を買う | PHT-427供給者 | PHT-427を購入する | PHT-427費用 | PHT-427生産者 | オーダーPHT-427 | PHT-427代理店