1. Autophagy
    PI3K/Akt/mTOR
  2. Autophagy
    PI3K

IITZ-01 

Cat. No.: HY-112897
Handling Instructions

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.

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

IITZ-01 Chemical Structure

IITZ-01 Chemical Structure

CAS No. : 1807988-47-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 680 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.

IC50 & Target

PI3Kγ

2.62 μM (IC50)

Autophagy

 

In Vitro

IITZ-01 shows negligible inhibition toward PI3Kγ (IC50: 2.62μM). Time-course immunoblotting experiment with IITZ-01-treated cells also displays significant elevation in SQSTM1 levels, indicating the autophagy inhibitory nature of the compound. In addition to that, both compounds IITZ-01 has demonstrated potent autophagy inhibitory activity in other breast, lung, and colon cancer cells[1].

In Vivo

Tumors after reaching ~100 mm3, vehicle, 45 mg/kg of IITZ-01, is administered through intraperitoneal (i.p.) route on every alternate day for 4 weeks. IITZ-01 reduces the active tumor burden around 8.8-fold, when compared with control group as determined by tumor photon counts. Moreover, tumor volume measurements have demonstrated that IITZ-01 has significantly inhibited average tumor growth when compared with control from third day of treatment. Significant reduction in average tumor weights is observed after treatment with IITZ-01 compared with control. This treatment schedule of both compounds is well tolerated in mice for the total duration of administration with no significant changes in their body weights[1].

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (310.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0725 mL 10.3625 mL 20.7250 mL
5 mM 0.4145 mL 2.0725 mL 4.1450 mL
10 mM 0.2072 mL 1.0362 mL 2.0725 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

  • 3.

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

    Solubility: 2.5 mg/mL (5.18 mM); Suspended solution; Need ultrasonic

References
Molecular Weight

482.51

Formula

C₂₆H₂₃FN₈O

CAS No.

1807988-47-1

SMILES

FC1=CC=C(NC2=NC(N3CCOCC3)=NC(NC4=CC=C(C5=NC6=CC=CC=C6N5)C=C4)=N2)C=C1

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
IITZ-01
Cat. No.:
HY-112897
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IITZ-01

Cat. No.: HY-112897