1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    c-Met/HGFR

TAS-115 mesylate (Synonyms: TAS-115 methanesulfonate)

Cat. No.: HY-12423A Purity: 99.15%
Handling Instructions

TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

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

TAS-115 mesylate Chemical Structure

TAS-115 mesylate Chemical Structure

CAS No. : 1688673-09-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 879 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

IC50 & Target

IC50: 30 nM (rVEGFR2), 32 nM (rMET)[1]

In Vitro

TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=0.032-0.362 μM) as a MET-targeted inhibitor. TAS-115 has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors[1]. Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells[2].

In Vivo

TAS-115 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 TAS-115. TAS-115 induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice[1].

Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (122.02 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution

References
Cell Assay
[2]

Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 μM) or erlotinib (0.3 μM) in the lower Transwell collagen–coated chambers are cocultured with MRC-5 (1000 cells/300 μL) cells in the upper chamber for 72 hours. The upper chamber is then removed. Cell viability is measured using the MTT assay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

The TAS-115 dose levels are set at 12.5, 50, and 200 mg/kg/d. The dose level for sunitinib is set at 40 mg/kg/d. Oral drug treatment is continued for 14 or 42 consecutive days for the chronic dosing in the SC-9 xenograft model. During the treatment period, TV and body weight are measured twice per week. The antitumor efficacy is assessed at the end of each study period[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

614.66

Formula

C₂₈H₂₇FN₄O₇S₂

CAS No.

1688673-09-7

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TAS-115 mesylate
Cat. No.:
HY-12423A
Quantity:

TAS-115 mesylate

Cat. No.: HY-12423A