Art. -Nr.: HY-13440

AMG 511

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.

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Reinheit: 99.76%
CAS. Nr.: 1253573-53-3
Formel: C₂₂H₂₈FN₉O₃S
Molecular Weight:517.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AMG 511 Chemical Structure

CAS. Nr.: 1253573-53-3

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PI3Kα

4 nM (Ki)

PI3Kβ

6 nM (Ki)

PI3Kδ

2 nM (Ki)

PI3Kγ

1 nM (Ki)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
U-87MG ATCC	ED₅₀	0.6 mg/kg Compound: 31	Antitumor activity against human U87MG cells xenografted in po dosed CD1 nude mouse administered QD for 12 days Antitumor activity against human U87MG cells xenografted in po dosed CD1 nude mouse administered QD for 12 days	[PMID: 22897589]
U-87MG ATCC	IC₅₀	0.004 μM Compound: 1, AMG 511	Inhibition of PI3K-mediated Akt S473 phosphorylation in human U87MG cells after 2 hrs by cell-based assay Inhibition of PI3K-mediated Akt S473 phosphorylation in human U87MG cells after 2 hrs by cell-based assay	[PMID: 25466188]
U-87MG ATCC	IC₅₀	4 nM Compound: 31	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human U87MG cells after 2 hrs Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human U87MG cells after 2 hrs	[PMID: 22897589]

In Vitro

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC₅₀ of 4 nM^[1].

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

In Vivo

AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days)^[1].
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile^[1].

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

Animal Model:

Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model^[1]
Dosage:

1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:

Oral administration, daily, for 12 days
Result:

Inhibited tumor growth.

Animal Model:

Male Sprague-Dawley rats^[1]
Dosage:

1 mg/kg
Administration:

Oral administration (Pharmacokinetic Analysis)
Result:

Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).

Chemical Information

CAS. Nr. 1253573-53-3
Appearance Solid
Molecular Weight 517.58
Formel C₂₂H₂₈FN₉O₃S
Color Light yellow to yellow
SMILES

NC1=NC(C2=CC([C@H](N3CCN(S(=O)(C)=O)CC3)C)=CN=C2NC4=CC(F)=C(OC)N=C4)=NC(C)=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (5)

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Journal Impact Factor

Cancer Discov

Discovery of BBO-11818, a Potent and Selective Noncovalent Inhibitor of (ON) and (OFF) KRAS with Activity against Multiple Oncogenic Mutants. [Abstract]

2026 Mar 6:OF1-OF20. PMID: 41790032
Leukemia

BET inhibitor-based combinations targeting novel dependencies in MECOM-rearranged (r) AML. [Abstract]

2025 Dec 19. PMID: 41419608
Cancer Lett

PI3K inhibitor impairs tumor progression and enhances sensitivity to anlotinib in anlotinib-resistant osteosarcoma. [Abstract]

2022 Jun 28;536:215660. PMID: 35318116
Phytomedicine

Gastrodin promotes Alkbh5 nuclear localization and Gclm m6A demethylation to alleviate ferroptosis in ischemic stroke. [Abstract]

2025 Aug 16:147:157177. PMID: 40839993
Exp Ther Med

Hydroxysafflor Yellow A inhibits the viability and migration of vascular smooth muscle cells induced by serum from rats with chronic renal failure via inactivation of the PI3K/Akt signaling pathway. [Abstract]

2021 Aug;22(2):850. PMID: 34149896

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9321 mL

9.6603 mL

19.3207 mL

5 mM

0.3864 mL

1.9321 mL

3.8641 mL

10 mM

0.1932 mL

0.9660 mL

1.9321 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: 2 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)
- Korean - KR (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)

Verweise

[1]. Mark H Norman, et al. Selective Class I Phosphoinositide 3-kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511. J Med Chem. 2012 Sep 13;55(17):7796-816. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9321 mL	9.6603 mL	19.3207 mL	48.3017 mL
	5 mM	0.3864 mL	1.9321 mL	3.8641 mL	9.6603 mL
	10 mM	0.1932 mL	0.9660 mL	1.9321 mL	4.8302 mL
	15 mM	0.1288 mL	0.6440 mL	1.2880 mL	3.2201 mL
	20 mM	0.0966 mL	0.4830 mL	0.9660 mL	2.4151 mL
	25 mM	0.0773 mL	0.3864 mL	0.7728 mL	1.9321 mL
	30 mM	0.0644 mL	0.3220 mL	0.6440 mL	1.6101 mL
	40 mM	0.0483 mL	0.2415 mL	0.4830 mL	1.2075 mL
	50 mM	0.0386 mL	0.1932 mL	0.3864 mL	0.9660 mL
	60 mM	0.0322 mL	0.1610 mL	0.3220 mL	0.8050 mL

Keywords

AMG 511

5 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) AMG 511

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 511 Related Classifications

HY-13440 Related Classifications