1. Protein Tyrosine Kinase/RTK
  2. IGF-1R
  3. PQ401

PQ401 

Cat. No.: HY-13686 Purity: 98.59%
Handling Instructions

PQ401, a selective insulin-like growth factor-1 receptor blocker, is a novel diarylurea compound that inhibits IGF1R autophosphorylation with IC50 < 1 uM.

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

PQ401 Chemical Structure

PQ401 Chemical Structure

CAS No. : 196868-63-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 127 In-stock
Estimated Time of Arrival: December 31
10 mg USD 115 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PQ401, a selective insulin-like growth factor-1 receptor blocker, is a novel diarylurea compound that inhibits IGF1R autophosphorylation with IC50 < 1 uM. IC50 Value: 12 uM (inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells) [1] Target: IGF1R in vitro: PQ401 inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells with an IC50 of 12 micromol/L and autophosphorylation of the isolated kinase domain of the IGF-IR with an IC50 <1 micromol/L. In addition,PQ401 inhibited the growth of cultured breast cancer cells in serum at 10 micromol/L. PQ401 was even more effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 micromol/L) [1]. Twenty-four hours of treatment with 15 micromol/L PQ401 induced caspase-mediated apoptosis. Pretreatment with PQ401 before IGF-1 (10 ng in 0.5 μl), both administered to the POA 30 min apart, showed significant attenuation of the IGF-1-induced increase in core body temperature (p < 0.05). A similar attenuated hyperthermic response to IGF-1 by PQ401 pretreatment is observed when the temperature of the BAT is measured [3]. in vivo: IGF1R inhibition by PQ401 exerted no significant effects on diabetic kidney disease parameters, arguing against a role for IGF-I in the pathogenesis of diabetic kidney disease. However, PQ401 affects normal kidneys, inducing renal hypertrophy as well as collagen and fat accumulation, with increased renal IGF-I mRNA, suggestive of a damage-regeneration process [2]. Clinical trial: No Development Reported

Molecular Weight

341.79

Formula

C₁₈H₁₆ClN₃O₂

CAS No.

196868-63-0

SMILES

O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=C(OC)C=CC(Cl)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (41.81 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9258 mL 14.6289 mL 29.2577 mL
5 mM 0.5852 mL 2.9258 mL 5.8515 mL
10 mM 0.2926 mL 1.4629 mL 2.9258 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.43 mg/mL (4.18 mM); Clear solution

  • 2.

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

    Solubility: 1.43 mg/mL (4.18 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 1.43 mg/mL (4.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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PQ401
Cat. No.:
HY-13686
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