2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. Ack1 Akt
  4. 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.

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Ack1 inhibitor 1 Chemical Structure

Ack1 inhibitor 1 Chemical Structure

CAS No. : 2924415-92-7

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Ack1 inhibitor 1 Related Antibodies

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Description

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[1].

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.

Ack1 inhibitor 1 Related Antibodies

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, Cmax 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].
. Hyzetimibe Pharmacokinetic Analysis in SD Rats [1]

SD大鼠体内药代动力学分析[1]

Route Dose (mg/kg) AUC0-∞ (ng•h/mL) t1/2 (h) Tmax (h) Cmax (μg/mL) Cl (mL/h/kg) F (%)
i.v. 2 1707.13 5.09 0.08 1429.26 19.85 /
p.o. 10 1920.56 7.71 6 119.52 / 19.8

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

727.77

Formula

C39H40F3N7O4
CAS No.
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

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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
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Purity & Documentation
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Ack1 inhibitor 1 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:

Ack1 inhibitor 12924415-92-7Ack1AktActivated Cdc42 kinase 1TNK2PKBProtein kinase Borally activeantitumorH1975 cells67R cellsInhibitorinhibitorinhibit

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