Cat. No.: HY-12340

ETP-46321

Customer Review

Based on 1 Customer Validation

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

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

Purity: 99.34%
CAS No.: 1252594-99-2
Formula: C₂₀H₂₇N₉O₃S
Molecular Weight:473.55

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ETP-46321 Chemical Structure

CAS No.: 1252594-99-2

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Sample (0.1mg)

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(In Japan)

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with K_iapps 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)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	IC₅₀	8.3 nM Compound: 14, ETP-46321	Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot	[PMID: 22520259]

In Vitro

ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (K_iapp=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 (K_iapp=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].

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

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].

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

Chemical Information

CAS No. 1252594-99-2
Appearance Solid
Molecular Weight 473.55
Formula C₂₀H₂₇N₉O₃S
Color White to off-white
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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 33 mg/mL (69.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

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Dilution Calculator

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Protocol

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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Martínez González S, et al. Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1117 mL	10.5585 mL	21.1171 mL	52.7927 mL
	5 mM	0.4223 mL	2.1117 mL	4.2234 mL	10.5585 mL
	10 mM	0.2112 mL	1.0559 mL	2.1117 mL	5.2793 mL
	15 mM	0.1408 mL	0.7039 mL	1.4078 mL	3.5195 mL
	20 mM	0.1056 mL	0.5279 mL	1.0559 mL	2.6396 mL
	25 mM	0.0845 mL	0.4223 mL	0.8447 mL	2.1117 mL
	30 mM	0.0704 mL	0.3520 mL	0.7039 mL	1.7598 mL
	40 mM	0.0528 mL	0.2640 mL	0.5279 mL	1.3198 mL
	50 mM	0.0422 mL	0.2112 mL	0.4223 mL	1.0559 mL
	60 mM	0.0352 mL	0.1760 mL	0.3520 mL	0.8799 mL

Keywords

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ETP-46321

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All PI3K Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ETP-46321 Related Classifications

Cat. No.: HY-12340