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Chemical Structure| 1035227-44-1 Chemical Structure| 1035227-44-1

Structure of AZ505 ditrifluoroacetate
CAS No.: 1035227-44-1

Chemical Structure| 1035227-44-1

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AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.

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Product Details of AZ505 ditrifluoroacetate

CAS No. :1035227-44-1
Formula : C33H40Cl2F6N4O8
M.W : 805.59
SMILES Code : O=C(N(C1CCCCC1)CCNCCC2=C(OCC(N3)=O)C3=C(O)C=C2)CCNCCC4=CC=C(Cl)C(Cl)=C4.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
MDL No. :MFCD28137733
InChI Key :LTZSXVZCRINTGV-UHFFFAOYSA-N
Pubchem ID :78357790

Safety of AZ505 ditrifluoroacetate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZ505 ditrifluoroacetate

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SPC-A1 cells 20 μM 24 hours AZ505 significantly inhibited the proliferation, migration, and invasion ability of SPC-A1 cells PMC8089105
GLC-82 cells 20 μM 24 hours AZ505 significantly inhibited the proliferation, migration, and invasion ability of GLC-82 cells PMC8089105
MDA-MB231 cells 20 μM 24 hours Induced cell apoptosis, inhibited cell migration and proliferation PMC5832424
MDA-MB468 cells 20 μM 24 hours Induced cell apoptosis, inhibited cell proliferation PMC5832424
HK-2 cells 20 μg/ml 24 hours To examine the role of SMYD2 in cisplatin-induced AKI, the results showed that SMYD2 siRNA inhibited cisplatin-induced kidney tubular cell injury and apoptosis PMC9421052
Rat renal interstitial fibroblasts (NRK-49F) 25 μM 36 hours Inhibited TGF-β1-induced activation of renal interstitial fibroblasts, reduced expression of α-SMA, fibronectin, and collagen I PMC9122037
HK-2 cells 100 µg/mL 48 hours To investigate the effect of COM stimulation on glycolysis in HK-2 cells, the results showed that COM stimulation increased the expression of glycolysis-related enzymes and elevated glycolysis levels PMC11504487
HaCaT cells 1.2 µM and 12 µM 6 hours inhibited BMP2-induced SMAD1/5 phosphorylation PMC5535043
HT-29 cells 10 µM 8 hours Decreased TMPRSS2 expression PMC9033063
Caco-2 cells 10 µM 8 hours Decreased TMPRSS2 expression PMC9033063

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse Pkd1nl/nl mouse model Intraperitoneal injection 5 mg/kg Once daily for 20 days To test the effect of AZ505 in delaying cyst growth in a Pkd1 mutant mouse model PMC5490754
BALB/c mice orthotopic xenograft model intraperitoneal injection 40 mg/kg every two days for 7 weeks AZ505 significantly attenuated tumor growth in the 786-O cell-implanted nude mice and suppressed Ki67 expression levels in the tumors compared to the control group. PMC6857066
BALB/c mice CT26 tumor model IP injection 20 mg/kg every other day from day 4 AZ505 treatment resulted in decreased tumor weight and tumor volume of CT26 cells in BALB/c mice with no decrease in body weight. In vivo flow data showed the increased tumor infiltration of CD8+ T cells. PMC10266737
BALB/c Nude mice subcutaneous xenograft model intraperitoneal injection 40 mg/kg once daily for 2 weeks AZ505 significantly inhibited tumor growth and metastasis PMC8089105
Nude mice TNBC cell xenograft model intraperitoneal injection 40 mg/kg once daily for 14 days Significantly inhibited tumor growth, reduced tumor cell proliferation and induced tumor cell apoptosis PMC5832424
C57/BL6 mice cisplatin-induced acute kidney injury model intraperitoneal injection 10 mg/kg once daily for 48 hours To investigate the protective effect of AZ505 on cisplatin-induced acute kidney injury, the results showed that AZ505 significantly improved kidney function, attenuated kidney tubular injury and inflammation, and promoted kidney tubular cell proliferation PMC9421052
C57 black mice Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 10 mg/kg Once daily for 6 days To evaluate the protective effect of AZ505 on UUO-induced renal fibrosis, results showed that AZ505 significantly reduced ECM deposition and expression of α-SMA, fibronectin, and collagen I PMC9122037
C57BL/6 black mice calcium oxalate stone mouse model intraperitoneal injection 10 mg/kg once daily for 12 days To investigate the effect of AZ505 on glycolysis, kidney injury, and fibrosis in a calcium oxalate stone mouse model, the results showed that AZ505 inhibited glycolysis and alleviated kidney injury and fibrosis PMC11504487

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.24mL

0.25mL

0.12mL

6.21mL

1.24mL

0.62mL

12.41mL

2.48mL

1.24mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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