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

ETP-45658 

Cat. No.: HY-110109 Purity: 98.05%
COA 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

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 187 In-stock
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10 mM * 1 mL in DMSO USD 187 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 170 In-stock
10 mg USD 280 In-stock
50 mg USD 850 In-stock
100 mg USD 1280 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ETP-45658 Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

ETP-45658 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

311.34

Appearance

Solid

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 MedChemExpress (MCE).
Purity & Documentation
References
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ETP-45658 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

ETP-456581198357-79-7ETP45658ETP 45658PI3KDNA-PKmTORPhosphoinositide 3-kinaseDNA-dependent protein kinaseMammalian target of RapamycinbreastcancerInhibitorinhibitorinhibit

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