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MedKoo Cat#: 526409 | Name: AZ-PFKFB3-67
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Chemical Structure

AZ-PFKFB3-67
AZ-PFKFB3-67
CAS#1704741-11-6

Theoretical Analysis

MedKoo Cat#: 526409

Name: AZ-PFKFB3-67

CAS#: 1704741-11-6

Chemical Formula: C26H25N5O3

Exact Mass: 455.1957

Molecular Weight: 455.52

Elemental Analysis: C, 68.56; H, 5.53; N, 15.37; O, 10.54

Price and Availability

Size Price Availability Quantity
10mg USD 450.00 2 Weeks
50mg USD 1,350.00 2 Weeks
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Related CAS #
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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/
Solvent mg/mL mM
Solubility
DMSO 45.6 100.00
Ethanol 45.6 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.