[CAS NO. 1688673-09-7] Pamufetinibmesylate
PRODUCTS SPECIFICATIONS [1688673-09-7]
DESCRIPTION [1688673-09-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 614.66 |
| Molecular Formula | C28H27FN4O7S2 |
| SMILES | CS(=O)(O)=O.O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3F)C2=C1)NC |
Summary
Pamufetinib (TAS-115) mesylate is a potent VEGFR and hepatocyte growth factor receptor ( c-Met/HGFR )-targeted kinase inhibitor, with IC 50 s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
IC50 & Target
IC50: 30 nM (rVEGFR2), 32 nM (rMET) [1]
In Vitro
Pamufetinib mesylate powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC 50 =0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI 50 =0.032-0.362 μM) as a MET-targeted inhibitor. Pamufetinib mesylate has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors [1] . Crizotinib and Pamufetinib mesylate inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pamufetinib mesylate completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of Pamufetinib mesylate. Pamufetinib mesylate induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04999761 | Taiho Pharmaceutical Co., Ltd. |
Advanced or Metastatic Solid Tumor|Pancreatic Ductal Adenocarcinoma|Colorectal Cancer|Non-small Cell Lung Cancer
|
June 1, 2021 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 75 mg/mL ( 122.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6269 mL | 8.1346 mL | 16.2692 mL |
| 5 mM | 0.3254 mL | 1.6269 mL | 3.2538 mL |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6269 mL |
References
- [1] Fujita H, et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol Cancer Ther. 2013 Dec;12(12):2685-96.
- [2] Nakade J, et al. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation. J Thorac Oncol. 2014 Jun;9(6):775-83.
