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Home > Products > Specialty & Industrial Chemicals > Specialty Chemicals > IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-Nμ-(2-methylquinolin-4-yl)urea
IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-Nμ-(2-methylquinolin-4-yl)urea structure, CAS 196868-63-0

IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-Nμ-(2-methylquinolin-4-yl)urea

CAS Number196868-63-0

Synonyms1-(5-Chloro-2-methoxyphenyl)-3-(2-methyl-4-quinolinyl)urea; 1-(5-Chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea; TCMDC-125497; N-(5-chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl); PQ 401; PQ401

Molecular FormulaC18H16ClN3O2

Molecular Weight341.792

Purity

Density1.4±0.1 g/cm3

Boiling Point426.1±45.0 °C at 760 mmHg

Melting Point190 °C(dec.)

Flash Point

Appearancewhite

EINECS

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Cat. No.: 2A-1170246 Purity:
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Quality Control of [ 196868-63-0 ] SDS Specification MoL

COA NMR CNMR HPLC LC-MS
Chemical & Physical Properties
CAS Number196868-63-0
Catalog No.2A-1170246
Chinese NamePQ401
Synonyms1-(5-Chloro-2-methoxyphenyl)-3-(2-methyl-4-quinolinyl)urea; 1-(5-Chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea; TCMDC-125497; N-(5-chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl); PQ 401; PQ401
Molecular FormulaC18H16ClN3O2
Molecular Weight341.792
Density1.4±0.1 g/cm3
Boiling Point426.1±45.0 °C at 760 mmHg
Melting Point190 °C(dec.)
Appearancewhite
Water SolubilityDMSO: >10mg/mL
Storage Condition2-8°C
ApplicationPQ401 is an IGF1R blocker that can inhibit IGF1R autophosphorylation with IC50 < 1 uM.
HTC2933499090
PubChem ID14720372
SMILESCOc1ccc(Cl)cc1NC(=O)Nc1cc(C)nc2ccccc12
InChIInChI=1S/C18H16ClN3O2/c1-11-9-15(13-5-3-4-6-14(13)20-11)21-18(23)22-16-10-12(19)7-8-17(16)24-2/h3-10H,1-2H3,(H2,20,21,22,23)
InChI KeyYBLWOZUPHDKFOT-UHFFFAOYSA-N
Hazard Symbolstransportation
BioactivityPQ401, 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: IGF1Rin 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 Related Catalog Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R Research Areas >> Cancer References [1]. Gable KL, Maddux BA, Penaranda C, Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86. [2]. Troib A, Landau D, Youngren JF, The effects of type 1 IGF receptor inhibition in a mouse model of diabetic kidney disease. Growth Horm IGF Res. 2011 Oct;21(5):285-91. [3]. Sanchez-Alavez M, Osborn O, Tabarean IV, Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem. 2011 Apr 29;286(17):14983-90. [4]. Youssif C, et al. Myeloid p38α signaling promotes intestinal IGF-1 production and inflammation-associated tumorigenesis. EMBO Mol Med. 2018 Jul;10(7). pii: e8403. Chemical & Physical Properties Density 1.4±0.1 g/cm3 Boiling Point 426.1±45.0 °C at 760 mmHg Melting Point 190 °C(dec.) Molecular Formula C18H16ClN3O2 Molecular Weight 341.792 Flash Point 211.5±28.7 °C Exact Mass 341.093109 PSA 63.25000 LogP 5.35 Appearance of Characters white Vapour Pressure 0.0±1.0 mmHg at 25°C Index of Refraction 1.709 InChIKey YBLWOZUPHDKFOT-UHFFFAOYSA-N SMILES COc1ccc(Cl)cc1NC(=O)Nc1cc(C)nc2ccccc12 Storage condition 2-8°C Water Solubility DMSO: >10mg/mL
Use ofProperties Name 1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea Synonym More Synonyms PQ 401 Biological Activity Related Catalog Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R Research Areas >> Cancer References [1]. Gable KL, Maddux BA, Penaranda C, Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86. [2]. Troib A, Landau D, Youngren JF, The effects of type 1 IGF receptor inhibition in a mouse model of diabetic kidney disease. Growth Horm IGF Res. 2011 Oct;21(5):285-91. [3]. Sanchez-Alavez M, Osborn O, Tabarean IV, Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem. 2011 Apr 29;286(17):14983-90. [4]. Youssif C, et al. Myeloid p38α signaling promotes intestinal IGF-1 production and inflammation-associated tumorigenesis. EMBO Mol Med. 2018 Jul;10(7). pii: e8403. Chemical & Physical Properties Exact Mass 341.093109 PSA 63.25000 Appearance of Characters white Index of Refraction 1.709 InChIKey YBLWOZUPHDKFOT-UHFFFAOYSA-N
Tax Rebate13.0%
SupervisionNone. MFN tariff: 6.5%. Ordinary tariff: 20.0%
Transport InfoProduct name: Purity: 99.0%
MSDS Transport InfoModule 14. Shipping information 14.1 UN number European Dangerous Regulations for land transport: 2811 International Dangerous Regulations for sea transport: 2811 International Dangerous Regulations for air transport: 2811 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: TOXIC SOLID, ORGANIC, N.O.S. (PQ401) IMDG: TOXIC SOLID, ORGANIC, N.O.S. (PQ401) International air transport hazard regulations: Toxic solid, organic, n.o.s. (PQ401) 14.3 Transport hazard categories European Land Transport Danger Regulations: 6.1 International Maritime Transport Danger Regulations: 6.1 International Air Transport Danger Regulations: 6.1 14.4 Package group European Land Transport Danger Regulations: III International Maritime Transport Danger Regulations: III International Air Transport Danger Regulations: III 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special reminder to users No data available
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