Product Details
| Product Name:
PRN1371 |
CAS No.:
1802929-43-6 |
| Purity:
99.72% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | PRN1371 |
| Description | PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R). |
| In vitro | PRN1371 exhibits high biochemical and cellular potency (FGFR1 IC50: 0.6 nM, SNU16 IC50: 2.6 nM), sustained target engagement (FGFR1 occupancy 24 h = 96%), less than 30% hERG inhibition at 1 μM, and favorable predicted ADME stability with BME reactivity Kd > 100 μM. |
| In vivo | In PK studies of rat, dog, and cynomolgus monkey, PRN1371show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing p.o (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirm the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant bodyweight loss. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 12 mg/mL (21.38 mM), Sonication and heating are recommended.
|
| Keywords | PRN 1371 | inhibit | CSF1R | Inhibitor | colony stimulating factor 1 receptor | c-Fms | PRN-1371 | CSF-1R | FGFR | CSF-1 receptor | Fibroblast growth factor receptor | PRN1371 |
| Inhibitors Related | Amlexanox | Nintedanib | PLX5622 | Sotuletinib | Ferulic Acid | Pexidartinib | Nintedanib esylate | Ponatinib | Formononetin | Lenvatinib mesylate | Erdafitinib | Pazopanib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States