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MedKoo Cat#: 407199 | Name: PQ401
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PQ401 is a potent and selective IGF-1R inhibitor. PQ-401 induces apoptosis and inhibits growth, proliferation and migration of glioma cells. PQ401 not only induced cellular apoptosis in U87MG cells and subsequently reduced cell viability and proliferation but also attenuated cell mobility in vitro. More importantly, through a mouse xenograft model, administration of PQ401 on mice led to suppression of glioma tumour growth in vivo. PQ401 may serve as a promising leading drug for treating glioma patients with elevated IGF-1R signalling.

Chemical Structure

PQ401
PQ401
CAS#196868-63-0

Theoretical Analysis

MedKoo Cat#: 407199

Name: PQ401

CAS#: 196868-63-0

Chemical Formula: C18H16ClN3O2

Exact Mass: 341.0931

Molecular Weight: 341.80

Elemental Analysis: C, 63.25; H, 4.72; Cl, 10.37; N, 12.29; O, 9.36

Price and Availability

Size Price Availability Quantity
10mg USD 110.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,850.00 Ready to ship
1g USD 3,950.00 Ready to Ship
2g USD 6,250.00 Ready to Ship
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Related CAS #
No Data
Synonym
PQ401; PQ-401; PQ 401.
IUPAC/Chemical Name
N-(5-Chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl)urea
InChi Key
YBLWOZUPHDKFOT-UHFFFAOYSA-N
InChi Code
InChI=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)
SMILES Code
O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=CC(Cl)=CC=C3OC
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
PQ401 is a potent inhibitor of IGF-IR signaling that inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM.
In vitro activity:
To access the effect of PQ401 on apoptosis induction in OS cells, U2OS cancer cells were treated with PQ401 at IC50 concentration (5 µM) and 10 µM, and then subjected to Annexin-V/PI staining and analysis by flow cytometry. It was observed that PQ401 induced apoptosis in a dose-dependent manner. The results clearly show that both early and late apoptosis were increased after PQ401 treatment (Figure 3B,3C). The cell migration capability was tested using wound healing and transwell assays. The findings demonstrated that OS cancer cell migration was significantly decreased with low concentrations of PQ401 (0.25 µM and 0.5 µM, Figure 4A,4C). The inhibition of cell migration at 0.5 µM was stronger than 0.25 µM in both wound healing and transwell assays (Figure 4B,4D). Colony formation inhibition by PQ401 was chosen to evaluate the effect of IGF-1R on clonogenesis. The findings show that the U2OS cell colony formation capability was significantly decreased with the treatment of PQ401 at the IC50 (5 µM) and at 10 µM (Figure 5B,5C). In addition, exposure of U2OS cells to 5 µM of PQ401 for 4 h resulted in a significant reduction in phosphorylation of IGF-1R and AKT (Figure 5E). Taken together, the results suggest that PQ401 may be a promising drug candidate for clinical chemotherapy for OS patients with metastasis. Reference: Int J Clin Exp Pathol. 2019; 12(5): 1589–1598. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6947108/
In vivo activity:
MCNeuA breast cancer cells were employed in a syngeneic mouse model of breast cancer. Thus, these cells were employed for in vivo studies to examine PQ401 effects against an aggressive tumor phenotype observed in ∼30% of human breast cancers that is recalcitrant to antiestrogen therapy. In addition, when these cells are implanted s.c. into the strain from which they were derived, all injected animals develop tumors. Thus, treatment could be initiated 3 days following implantation, before the development of palpable tumors. Injection of either 50 or 100 mg/kg PQ401 thrice per week in a polysorbate 80/ethanol vehicle resulted in a significant dosedependent reduction in tumor growth over the course of the study (Fig. 7 ). Tumor growth in the animals treated with 100 mg/kg PQ401 thrice a week was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals. In summary, a novel class of IGF-IR-inhibiting compounds have been identified that are potential anticancer agents. The lead diaryl urea compound, PQ401, inhibits growth of MCF-7 breast cancer cells both in culture and in a syngeneic mouse model of breast cancer. PQ401 acts, at least in part, by inducing caspase-mediated apoptosis via inhibition of the Akt/protein kinase B pathway. Reference: Mol Cancer Ther. 2006 Apr;5(4):1079-86. https://mct.aacrjournals.org/content/5/4/1079.long
Solvent mg/mL mM comments
Solubility
Ethanol 8.5 24.90
DMSO 17.0 49.70
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 341.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Qi B, Zhang R, Sun R, Guo M, Zhang M, Wei G, Zhang L, Yu S, Huang H. IGF-1R inhibitor PQ401 inhibits osteosarcoma cell proliferation, migration and colony formation. Int J Clin Exp Pathol. 2019 May 1;12(5):1589-1598. PMID: 31933976; PMCID: PMC6947108. 2. Zhou X, Zhao X, Li X, Ping G, Pei S, Chen M, Wang Z, Zhou W, Jin B. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J Chemother. 2016;28(1):44-9. doi: 10.1179/1973947815Y.0000000026. PMID: 25971682. 3. Gable KL, Maddux BA, Penaranda C, Zavodovskaya M, Campbell MJ, Lobo M, Robinson L, Schow S, Kerner JA, Goldfine ID, Youngren JF. 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. doi: 10.1158/1535-7163.MCT-05-0397. PMID: 16648580.
In vitro protocol:
1. Qi B, Zhang R, Sun R, Guo M, Zhang M, Wei G, Zhang L, Yu S, Huang H. IGF-1R inhibitor PQ401 inhibits osteosarcoma cell proliferation, migration and colony formation. Int J Clin Exp Pathol. 2019 May 1;12(5):1589-1598. PMID: 31933976; PMCID: PMC6947108. 2. Zhou X, Zhao X, Li X, Ping G, Pei S, Chen M, Wang Z, Zhou W, Jin B. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J Chemother. 2016;28(1):44-9. doi: 10.1179/1973947815Y.0000000026. PMID: 25971682.
In vivo protocol:
1. Gable KL, Maddux BA, Penaranda C, Zavodovskaya M, Campbell MJ, Lobo M, Robinson L, Schow S, Kerner JA, Goldfine ID, Youngren JF. 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. doi: 10.1158/1535-7163.MCT-05-0397. PMID: 16648580. 2. Zhou X, Zhao X, Li X, Ping G, Pei S, Chen M, Wang Z, Zhou W, Jin B. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J Chemother. 2016;28(1):44-9. doi: 10.1179/1973947815Y.0000000026. PMID: 25971682.
1: Vong CT, Tan D, Liao F, Chen Z, Chen Z, Tseng HHL, Cheang WS, Wang S, Wang Y. Ginsenoside Rk1 Ameliorates ER Stress-Induced Apoptosis through Directly Activating IGF-1R in Mouse Pancreatic [Formula: see text]-Cells and Diabetic Pancreas. Am J Chin Med. 2024;52(4):1195-1211. doi: 10.1142/S0192415X24500484. Epub 2024 May 27. PMID: 38798150. 2: Li J, Zhou X, Chen J, Eliasson P, Kingham PJ, Backman LJ. Secretome from myoblasts statically loaded at low intensity promotes tenocyte proliferation via the IGF-1 receptor pathway. FASEB J. 2023 Oct;37(10):e23203. doi: 10.1096/fj.202301097R. PMID: 37732638. 3: Ye Q, Hickey J, Summers K, Falatovich B, Gencheva M, Eubank TD, Ivanov AV, Guo NL. Multi-Omics Immune Interaction Networks in Lung Cancer Tumorigenesis, Proliferation, and Survival. Int J Mol Sci. 2022 Nov 29;23(23):14978. doi: 10.3390/ijms232314978. PMID: 36499305; PMCID: PMC9738413. 4: Kim W, Zou G, Pan W, Fricke N, Faizi HA, Kim SM, Khader R, Li S, Lee K, Escorba I, Vlahovska PM, Gao H, Ausubel FM, Mylonakis E. The Neutrally Charged Diarylurea Compound PQ401 Kills Antibiotic-Resistant and Antibiotic-Tolerant Staphylococcus aureus. mBio. 2020 Jun 30;11(3):e01140-20. doi: 10.1128/mBio.01140-20. PMID: 32605985; PMCID: PMC7327171. 5: Qi B, Zhang R, Sun R, Guo M, Zhang M, Wei G, Zhang L, Yu S, Huang H. IGF-1R inhibitor PQ401 inhibits osteosarcoma cell proliferation, migration and colony formation. Int J Clin Exp Pathol. 2019 May 1;12(5):1589-1598. PMID: 31933976; PMCID: PMC6947108. 6: Alyoussef A. The therapeutic effects of blocking IGF-R1 on mice model of skin cancer. J Dermatolog Treat. 2021 Nov;32(7):803-811. doi: 10.1080/09546634.2019.1708243. Epub 2020 Jan 3. PMID: 31868059. 7: Tomilov A, Allen S, Hui CK, Bettaieb A, Cortopassi G. Idebenone is a cytoprotective insulin sensitizer whose mechanism is Shc inhibition. Pharmacol Res. 2018 Nov;137:89-103. doi: 10.1016/j.phrs.2018.09.024. Epub 2018 Oct 2. PMID: 30290222. 8: Yang ZQ, Zhang HL, Duan CC, Geng S, Wang K, Yu HF, Yue ZP, Guo B. IGF1 regulates RUNX1 expression via IRS1/2: Implications for antler chondrocyte differentiation. Cell Cycle. 2017 Mar 19;16(6):522-532. doi: 10.1080/15384101.2016.1274471. Epub 2017 Jan 5. PMID: 28055425; PMCID: PMC5384582. 9: Shi Y, He MX. PfIRR Interacts with HrIGF-I and Activates the MAP-kinase and PI3-kinase Signaling Pathways to Regulate Glycogen Metabolism in Pinctada fucata. Sci Rep. 2016 Feb 25;6:22063. doi: 10.1038/srep22063. PMID: 26911653; PMCID: PMC4766514. 10: Zhou X, Zhao X, Li X, Ping G, Pei S, Chen M, Wang Z, Zhou W, Jin B. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J Chemother. 2016;28(1):44-9. doi: 10.1179/1973947815Y.0000000026. PMID: 25971682. 11: Wang H, Qin J, Gong S, Feng B, Zhang Y, Tao J. Insulin-like growth factor-1 receptor-mediated inhibition of A-type K(+) current induces sensory neuronal hyperexcitability through the phosphatidylinositol 3-kinase and extracellular signal-regulated kinase 1/2 pathways, independently of Akt. Endocrinology. 2014 Jan;155(1):168-79. doi: 10.1210/en.2013-1559. Epub 2013 Dec 20. PMID: 24080365. 12: Ghosh MC, Gorantla V, Makena PS, Luellen C, Sinclair SE, Schwingshackl A, Waters CM. Insulin-like growth factor-I stimulates differentiation of ATII cells to ATI-like cells through activation of Wnt5a. Am J Physiol Lung Cell Mol Physiol. 2013 Aug 1;305(3):L222-8. doi: 10.1152/ajplung.00014.2013. Epub 2013 May 24. PMID: 23709620; PMCID: PMC3743013. 13: Jameson MJ, Beckler AD, Taniguchi LE, Allak A, Vanwagner LB, Lee NG, Thomsen WC, Hubbard MA, Thomas CY. Activation of the insulin-like growth factor-1 receptor induces resistance to epidermal growth factor receptor antagonism in head and neck squamous carcinoma cells. Mol Cancer Ther. 2011 Nov;10(11):2124-34. doi: 10.1158/1535-7163.MCT-11-0294. Epub 2011 Aug 30. PMID: 21878657; PMCID: PMC3213311. 14: Troib A, Landau D, Youngren JF, Kachko L, Rabkin R, Segev Y. 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. doi: 10.1016/j.ghir.2011.07.007. Epub 2011 Aug 23. PMID: 21865067; PMCID: PMC4238882. 15: Sanchez-Alavez M, Osborn O, Tabarean IV, Holmberg KH, Eberwine J, Kahn CR, Bartfai T. Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem. 2011 Apr 29;286(17):14983-90. doi: 10.1074/jbc.M110.188540. Epub 2011 Feb 17. PMID: 21330367; PMCID: PMC3083203. 16: Lai VK, Linares-Palomino J, Nadal-Ginard B, Galiñanes M. Bone marrow cell- induced protection of the human myocardium: characterization and mechanism of action. J Thorac Cardiovasc Surg. 2009 Dec;138(6):1400-08.e1. doi: 10.1016/j.jtcvs.2009.07.013. Epub 2009 Aug 18. PMID: 19692000. 17: Sivakumar R, Koga H, Selvendiran K, Maeyama M, Ueno T, Sata M. Autocrine loop for IGF-I receptor signaling in SLUG-mediated epithelial-mesenchymal transition. Int J Oncol. 2009 Feb;34(2):329-38. PMID: 19148466. 18: Gable KL, Maddux BA, Penaranda C, Zavodovskaya M, Campbell MJ, Lobo M, Robinson L, Schow S, Kerner JA, Goldfine ID, Youngren JF. 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. doi: 10.1158/1535-7163.MCT-05-0397. PMID: 16648580.