ETP-46321

Cat. No.: HY-12340 Purity: 99.34%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

ETP-46321 Chemical Structure

CAS No. : 1252594-99-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 253	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 253	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 63	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1330	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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•Related Screening Libraries:

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

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.

Molecular Weight

473.55

Formula

C₂₀H₂₇N₉O₃S

CAS No.

1252594-99-2

Appearance

Solid

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.

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.34%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (88 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]

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	[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]

Complete Stock Solution Preparation Table

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

ETP-46321 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.

Keywords:

ETP-463211252594-99-2ETP46321ETP 46321PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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