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Cat. No.: HY-149989

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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.

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

CAS No.: 2924415-92-7
Formula: C₃₉H₄₀F₃N₇O₄
Molecular Weight:727.77

Storage:

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

Data Sheet (274 KB)

Ack1 inhibitor 1 Chemical Structure

CAS No.: 2924415-92-7

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vivo
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Akt Isoforms :

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 No. 2924415-92-7
Molecular Weight 727.77
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Solvent & Solubility

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:

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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

Purity & Documentation

Select Batch:

Purity: 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)

References

[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

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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.

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100 mg

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