country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-149989

Copy Link Print Information

Ack1 inhibitor 1

Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC₅₀ value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2924415-92-7
Formel: C₃₉H₄₀F₃N₇O₄
Molecular Weight:727.77

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Ack1 inhibitor 1 Chemical Structure

CAS. Nr.: 2924415-92-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vivo
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1975	IC₅₀	4.18 nM Compound: 10zi	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by SRB colorimetric assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by SRB colorimetric assay	[PMID: 37134203]

In Vitro

Ack1 inhibitor 1 inhibits of cell growth with IC₅₀s of 3.71 μM and 4.18 μM in 67R and H1975 cells^[1].
Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) alone or in combination with ASK120067 enhances antitumor effects in 67R^[1].
Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) inhibits the phosphorylation of ACK1 and AKT in 67R cells in a dose-dependent manner^[1].

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

Cell Viability Assay^[1]

Cell Line:

67R cells (ASK120067-resistant cells obtained from parental H1975 cells by a dose escalation method).
Concentration:

0-5000 nM (combined with ASK120067)
Incubation Time:

72 h
Result:

Caused strong synergistic anti-growth effects on 67R cells with high synergy scores of 10.83, respectively

Western Blot Analysis^[1]

Cell Line:

67R cells
Concentration:

1 μM and 5 μM
Incubation Time:

6 h (stimulated with or without EGF for 30 min)
Result:

Caused moderate down-regulation of p-ACK1 and p-AKT at 1 μM.
Exhibited better potency against p-AKT, while it was unable to completely inhibit p-ACK1 at 5 μM.

In Vivo

Ack1 inhibitor 1 (Compound 10zi) (10 mg/kg; PO; single dose) improves AUC value of 1920.56 h ng/mL, C_max of 119.52 μg/L, and an oral bioavailability of 19.80% in a single oral dose of 10 mg/kg in SD rats^[1].

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

Chemical Information

CAS. Nr. 2924415-92-7
Molecular Weight 727.77
Formel C₃₉H₄₀F₃N₇O₄
SMILES

CN(CC1)CCN1C(C=C2)=CC(OCC)=C2NC3=NC=C4C(N(C[C@@H]5OCCC5)C(C(C6=CC(NC(C7=CC(C(F)(F)F)=CC=C7)=O)=CC=C6)=C4)=O)=N3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Lösungsmittel & Löslichkeit

View the Complete Stock Solution Preparation Table

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Ack1 inhibitor 1 dissolve in 5% DMSO + 10% Solutol + 85% (10% HP-β-CD in Saline)^[1]

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.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Li Q, et al. Design, Synthesis, and Evaluation of (R)-8-((Tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as Novel Selective ACK1 Inhibitors to Combat Acquired Resistance to the Third-Generation EGFR Inhibitor. J Med Chem. 2023 May 25;66(10):6905-6921. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vivo
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Ack1 inhibitor 1

Alle Akt Isoform-spezifische Produkte anzeigen