1. PI3K/Akt/mTOR
    Cell Cycle/DNA Damage
  2. PI3K
    DNA-PK
    mTOR
  3. ETP-45658

ETP-45658 

Cat. No.: HY-110109 Purity: 98.05%
Handling Instructions

ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer.

For research use only. We do not sell to patients.

ETP-45658 Chemical Structure

ETP-45658 Chemical Structure

CAS No. : 1198357-79-7

Size Price Stock Quantity
5 mg USD 170 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer[1][2].

IC50 & Target[1]

PI3Kα

22.0 nM (IC50)

PI3Kδ

39.8 nM (IC50)

PI3Kβ

129.0 nM (IC50)

PI3Kγ

717.3 nM (IC50)

DNA-PK

70.6 nM (IC50)

mTOR

152.0 nM (IC50)

In Vitro

ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells[1].
ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively[1].
ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells[1].
ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively[1].
ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells[1].
ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: U2OS cells
Concentration: 10 μM
Incubation Time: 4 hours
Result: Caused a 95% decrease in the phosphorylation of FOXO3a at threonine 32 and a 55% reduction on Gsk3-β at serine 9.
Reduced the phosphorylation of the mTOR substrate p70 S6K.
In Vivo

ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

311.34

Formula

C16H17N5O2

CAS No.
SMILES

CN1C2=NC(C3=CC(O)=CC=C3)=NC(N4CCOCC4)=C2C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (802.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2119 mL 16.0596 mL 32.1192 mL
5 mM 0.6424 mL 3.2119 mL 6.4238 mL
10 mM 0.3212 mL 1.6060 mL 3.2119 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Product Name:
ETP-45658
Cat. No.:
HY-110109
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