WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H202722
CAS#: 1005780-62-0
Description: TAK-593 is a n oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity. TAK-593 selectively binds to and inhibits VEGFR and PDGFR, which may result in the inhibition of angiogenesis and tumor cell proliferation.
Hodoodo Cat#: H202722
Name: TAK-593
CAS#: 1005780-62-0
Chemical Formula: C23H23N7O3
Exact Mass: 445.19
Molecular Weight: 445.474
Elemental Analysis: C, 62.01; H, 5.20; N, 22.01; O, 10.77
Synonym: TAK593, TAK593, TAK 593
IUPAC/Chemical Name: N-(5-((2-(cyclopropanecarboxamido)imidazo[1,2-b]pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide
InChi Key: DZFZXPPHBWCXPQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H23N7O3/c1-13-4-7-16(11-17(13)24-23(32)18-10-14(2)27-29(18)3)33-21-9-8-20-25-19(12-30(20)28-21)26-22(31)15-5-6-15/h4,7-12,15H,5-6H2,1-3H3,(H,24,32)(H,26,31)
SMILES Code: O=C(C1=CC(C)=NN1C)NC2=CC(OC3=NN4C(C=C3)=NC(NC(C5CC5)=O)=C4)=CC=C2C
Appearance: 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: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 445.47 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: |
1: Miyamoto N, Sakai N, Hirayama T, Miwa K, Oguro Y, Oki H, Okada K, Takagi T, Iwata H, Awazu Y, Yamasaki S, Takeuchi T, Miki H, Hori A, Imamura S. Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylph enyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. Bioorg Med Chem. 2013 Apr 15;21(8):2333-45. doi: 10.1016/j.bmc.2013.01.074. Epub 2013 Feb 13. PubMed PMID: 23498918.
2: Awazu Y, Mizutani A, Nagase Y, Tsuchiya S, Nakamura K, Kakoi Y, Kitahara O, Takeuchi T, Yamasaki S, Miyamoto N, Iwata H, Miki H, Imamura S, Hori A. Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013 Apr;104(4):486-94. doi: 10.1111/cas.12101. Epub 2013 Feb 18. PubMed PMID: 23305239.
3: Iwata H, Imamura S, Hori A, Hixon MS, Kimura H, Miki H. Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51. doi: 10.1021/bi101777f. Epub 2011 Jan 10. PubMed PMID: 21182308.
