1. PI3K/Akt/mTOR
  2. PI3K
  3. ETP-46321

ETP-46321 

Cat. No.: HY-12340 Purity: 99.65%
Handling Instructions

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.

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

ETP-46321 Chemical Structure

ETP-46321 Chemical Structure

CAS No. : 1252594-99-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Description

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.

IC50 & Target[1]

p110α

2.3 nM (Ki)

PI3Kα-E545K

1.77 nM (Ki)

PI3Kα-E542K

1.89 nM (Ki)

PI3Kα-H1047R

2.33 nM (Ki)

p110δ

14.2 nM (Ki)

p110β

170 nM (Ki)

p110γ

179 nM (Ki)

In Vitro

ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (Kiapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC50 of 8.3 nM[1].

In Vivo

ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques[1].

Molecular Weight

473.55

Formula

C₂₀H₂₇N₉O₃S

CAS No.

1252594-99-2

SMILES

NC(N=C1)=NC=C1C2=CN3C=C(CN4CCN(S(=O)(C)=O)CC4)N=C3C(N5CCOCC5)=N2

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 : ≥ 33 mg/mL (69.69 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1117 mL 10.5585 mL 21.1171 mL
5 mM 0.4223 mL 2.1117 mL 4.2234 mL
10 mM 0.2112 mL 1.0559 mL 2.1117 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
BALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.

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

References
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Keywords:

ETP-46321ETP46321ETP 46321PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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