MedKoo Biosciences

TAS-115 mesylate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 207092

CAS#: 1688673-09-7 (mesylate)

Description: TAS-115 is a c-MET Inhibitor. TAS-115 inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. TAS-115 is extremely selective and specific, at least in vitro. In in vivo studies, TAS-115 completely suppressed 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 induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity.

Chemical Structure

TAS-115 mesylate

CAS# 1688673-09-7 (mesylate)

Instruction

Theoretical Analysis

MedKoo Cat#: 207092
Name: TAS-115 mesylate
CAS#: 1688673-09-7 (mesylate)
Chemical Formula: C28H27FN4O7S2
Exact Mass: 0.00
Molecular Weight: 614.663
Elemental Analysis: C, 54.71; H, 4.43; F, 3.09; N, 9.12; O, 18.22; S, 10.43

Price and Availability

Size	Price	Availability
50mg	USD 950	2 Weeks
100mg	USD 1650	2 Weeks
200mg	USD 2650	2 Weeks
500mg	USD 3650	2 Weeks
1g	USD 4650	2 Weeks
2g	USD 7650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: TAS115 mesylate; TAS115; TAS-115; TAS 115; Pamufetinib mesylate; Pamufetinib (mesylate); Pamufetinib mesilate

IUPAC/Chemical Name: 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide methanesulfonate

InChi Key: NUYQWFCUOAVQAL-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H23FN4O4S.CH4O3S/c1-29-26(34)19-14-18-21(15-24(19)35-2)30-11-10-22(18)36-23-9-8-17(13-20(23)28)31-27(37)32-25(33)12-16-6-4-3-5-7-16;1-5(2,3)4/h3-11,13-15H,12H2,1-2H3,(H,29,34)(H2,31,32,33,37);1H3,(H,2,3,4)

SMILES Code: 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.OS(=O)(C)=O

Appearance: 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

Shelf Life: >3 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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 614.66 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.

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:
In vitro protocol:
In vivo protocol:

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1: Koyama K, Goto H, Morizumi S, Kagawa K, Nishimura H, Sato S, Kawano H, Toyoda Y, Ogawa H, Homma S, Nishioka Y. The Tyrosine Kinase Inhibitor TAS-115 Attenuates Bleomycin-induced Lung Fibrosis in Mice. Am J Respir Cell Mol Biol. 2019 Apr;60(4):478-487. doi: 10.1165/rcmb.2018-0098OC. PubMed PMID: 30540913.

2: Yamada S, Imura Y, Nakai T, Nakai S, Yasuda N, Kaneko K, Outani H, Takenaka S, Hamada K, Myoui A, Araki N, Ueda T, Itoh K, Yoshikawa H, Naka N. Therapeutic potential of TAS-115 via c-MET and PDGFRα signal inhibition for synovial sarcoma. BMC Cancer. 2017 May 16;17(1):334. doi: 10.1186/s12885-017-3324-3. PubMed PMID: 28511645; PubMed Central PMCID: PMC5434537.

3: Fujita H, Gomori A, Fujioka Y, Kataoka Y, Tanaka K, Hashimoto A, Suzuki T, Ito K, Haruma T, Yamamoto-Yokoi H, Harada N, Sakuragi M, Oda N, Matsuo K, Inada M, Yonekura K. High Potency VEGFRs/MET/FMS Triple Blockade by TAS-115 Concomitantly Suppresses Tumor Progression and Bone Destruction in Tumor-Induced Bone Disease Model with Lung Carcinoma Cells. PLoS One. 2016 Oct 13;11(10):e0164830. doi: 10.1371/journal.pone.0164830. eCollection 2016. PubMed PMID: 27736957; PubMed Central PMCID: PMC5063576.

4: Watanabe K, Hirata M, Tominari T, Matsumoto C, Fujita H, Yonekura K, Murphy G, Nagase H, Miyaura C, Inada M. The MET/Vascular Endothelial Growth Factor Receptor (VEGFR)-targeted Tyrosine Kinase Inhibitor Also Attenuates FMS-dependent Osteoclast Differentiation and Bone Destruction Induced by Prostate Cancer. J Biol Chem. 2016 Sep 30;291(40):20891-20899. Epub 2016 Aug 18. PubMed PMID: 27539855; PubMed Central PMCID: PMC5076502.

5: Kunii E, Ozasa H, Oguri T, Maeno K, Fukuda S, Uemura T, Takakuwa O, Ohkubo H, Takemura M, Niimi A. Reversal of c-MET-mediated Resistance to Cytotoxic Anticancer Drugs by a Novel c-MET Inhibitor TAS-115. Anticancer Res. 2015 Oct;35(10):5241-7. PubMed PMID: 26408683.

6: Nakade J, Takeuchi S, Nakagawa T, Ishikawa D, Sano T, Nanjo S, Yamada T, Ebi H, Zhao L, Yasumoto K, Matsumoto K, Yonekura K, Yano S. 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. doi: 10.1097/JTO.0000000000000170. PubMed PMID: 24828661; PubMed Central PMCID: PMC4132034.

7: Fujita H, Miyadera K, Kato M, Fujioka Y, Ochiiwa H, Huang J, Ito K, Aoyagi Y, Takenaka T, Suzuki T, Ito S, Hashimoto A, Suefuji T, Egami K, Kazuno H, Suda Y, Nishio K, Yonekura K. 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. doi: 10.1158/1535-7163.MCT-13-0459. Epub 2013 Oct 18. PubMed PMID: 24140932.

8: Zhao L, Yasumoto K, Kawashima A, Nakagawa T, Takeuchi S, Yamada T, Matsumoto K, Yonekura K, Yoshie O, Yano S. Paracrine activation of MET promotes peritoneal carcinomatosis in scirrhous gastric cancer. Cancer Sci. 2013 Dec;104(12):1640-6. doi: 10.1111/cas.12301. Epub 2013 Nov 13. PubMed PMID: 24118504.

9: Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53. doi: 10.1093/jjco/hyt131. Epub 2013 Sep 5. PubMed PMID: 24014883; PubMed Central PMCID: PMC3787805.

10: Belleville I, Vaillant G, Farnier M, Brun JM. [Influence of acute hyperinsulinism on arterial pressure of diabetics. Reproducibility of the hypotensive effect]. Arch Mal Coeur Vaiss. 1988 Jun;81 Spec No:79-82. French. PubMed PMID: 3142434.

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