AZ-PFKFB3-67
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526409

CAS#: 1704741-11-6

Description: AZ-PFKFB3-67 is a novel potent and selective PFKFB3 inhibitor.

Chemical Structure

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AZ-PFKFB3-67
CAS# 1704741-11-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526409
Name: AZ-PFKFB3-67
CAS#: 1704741-11-6
Chemical Formula: C26H25N5O3
Exact Mass: 455.20
Molecular Weight: 455.518
Elemental Analysis: C, 68.56; H, 5.53; N, 15.37; O, 10.54

Price and Availability

Size Price Availability Quantity
10mg USD 255
50mg USD 985
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Synonym: AZ-PFKFB3-67; AZ-PFKFB367; AZ-PFKFB3 67; AZ-PFKFB 367; AZ-PFKFB-367; AZPFKFB-367; AZPFKFB367; AZPFKFB 367;

IUPAC/Chemical Name: (2S)-N-[4-[[3-Cyano-1-[(3,5-dimethyl-4-isoxazolyl)methyl]-1H-indol-5-yl]oxy]phenyl]-2-pyrrolidinecarboxamide

InChi Key: NDIKFKQBWGMLCA-DEOSSOPVSA-N

InChi Code: InChI=1S/C26H25N5O3/c1-16-23(17(2)34-30-16)15-31-14-18(13-27)22-12-21(9-10-25(22)31)33-20-7-5-19(6-8-20)29-26(32)24-4-3-11-28-24/h5-10,12,14,24,28H,3-4,11,15H2,1-2H3,(H,29,32)/t24-/m0/s1

SMILES Code: O=C([C@H]1NCCC1)NC2=CC=C(OC3=CC4=C(N(CC5=C(C)ON=C5C)C=C4C#N)C=C3)C=C2

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 to 100 mM in DMSO and to 100 mM in ethanol

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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: AZ-PFKFB3-67 is a PFKFB3 kinase inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively.
In vitro activity: As PFKFB3 protein expression was highest upon TNF-α and DMOG stimulation/treatment, these two conditions were explored further for this experiment. Interestingly, upon TNF-α stimulation and AZ67 treatment, a significant reduction in tube and mesh structure formation was observed (Figure 5A). Reference: Int J Mol Sci. 2021 Jun; 22(11): 5970. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8198190/
In vivo activity: Finally, this study aimed to elucidate whether pharmacological inhibition of PFKFB3 by AZ67 would result in the expected in vivo effects for neovessel formation. Considered as the standard method for in vivo evaluation of pro- and anti-angiogenic compounds, the Matrigel plug assay revealed that AZ67 significantly inhibited new vessel formation in C57BL/6 mice. Fourteen days after implantation, the Matrigel plug containing the vehicle formed a large blood vessel network connected with the host vasculature, with the vessel containing blood, as seen in (Figure 6A) (red structures). In contrast, the Matrigel plug containing AZ67 displayed no functional vessels. This was further represented by microscopic images of CD31 positive vessel structures (in brown), accompanied by the quantification (Figure 6B). Reference: Int J Mol Sci. 2021 Jun; 22(11): 5970. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8198190/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.6 100.00
Ethanol 45.6 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 455.52 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.

Recalculate based on batch purity %
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: 1. Emini Veseli B, Van Wielendaele P, Delibegovic M, Martinet W, De Meyer GRY. The PFKFB3 Inhibitor AZ67 Inhibits Angiogenesis Independently of Glycolysis Inhibition. Int J Mol Sci. 2021 May 31;22(11):5970. doi: 10.3390/ijms22115970. PMID: 34073144; PMCID: PMC8198190.
In vitro protocol: 1. Emini Veseli B, Van Wielendaele P, Delibegovic M, Martinet W, De Meyer GRY. The PFKFB3 Inhibitor AZ67 Inhibits Angiogenesis Independently of Glycolysis Inhibition. Int J Mol Sci. 2021 May 31;22(11):5970. doi: 10.3390/ijms22115970. PMID: 34073144; PMCID: PMC8198190.
In vivo protocol: 1. Emini Veseli B, Van Wielendaele P, Delibegovic M, Martinet W, De Meyer GRY. The PFKFB3 Inhibitor AZ67 Inhibits Angiogenesis Independently of Glycolysis Inhibition. Int J Mol Sci. 2021 May 31;22(11):5970. doi: 10.3390/ijms22115970. PMID: 34073144; PMCID: PMC8198190.

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