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Chemical Structure| 1035227-43-0 Chemical Structure| 1035227-43-0

Structure of AZ505
CAS No.: 1035227-43-0

Chemical Structure| 1035227-43-0

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AZ505 exhibits potent and selective inhibition against SMYD2, with an IC50 of 0.12 μM.

Synonyms: AZ505

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Product Details of AZ505

CAS No. :1035227-43-0
Formula : C29H38Cl2N4O4
M.W : 577.54
SMILES Code : O=C(N(C1CCCCC1)CCNCCC2=C(OCC(N3)=O)C3=C(O)C=C2)CCNCCC4=CC=C(Cl)C(Cl)=C4
Synonyms :
AZ505
MDL No. :N/A

Safety of AZ505

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

Related Pathways of AZ505

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HaCaT cells 1.2 and 12 µM 6 hours Inhibited BMP2-induced SMAD1/5 phosphorylation J Biol Chem. 2017 Jul 28;292(30):12702-12712.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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, results showed that AZ505 significantly improved kidney function, attenuated kidney tubular injury and inflammation, and promoted kidney tubular cell proliferation. Front Pharmacol. 2022 Aug 15;13:829630.
C57 black mice Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 10 mg/kg Once daily for 6 days To evaluate the effect of AZ505 on UUO-induced renal fibrosis, results showed that AZ505 significantly reduced ECM deposition and activation of renal interstitial fibroblasts FASEB J. 2021 Jul;35(7):e21715.
C57BL/6 black mice Glyoxylate-induced CaOx stone mice model Intraperitoneal injection 10 mg/kg Once daily for 12 consecutive days AZ505 inhibited SMYD2 expression, reduced CaOx crystal formation, kidney damage, and fibrosis, and alleviated inflammation. Biomedicines. 2024 Oct 8;12(10):2279.
BALB/c mice CT26 tumor model IP injection 20 mg/kg Every other day at a dose of 20 mg/kg 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. This demonstrated that the SMYD2 inhibitor has no overt toxicity but high efficiency. Sci Adv. 2023 Jun 16;9(24):eade6624
BALB/c Nude mice Lung cancer xenograft model Intraperitoneal injection 40 mg/kg Once daily for two weeks Inhibited tumor growth and metastasis Cell Death Dis. 2021 May 2;12(5):439.
Nude mice MDA-MB231 xenograft model Intraperitoneal injection 40 mg/kg Daily for 14 days Significantly retarded tumor growth Cell Death Dis. 2018 Feb 27;9(3):326.
Nude mice Orthotopic xenograft model using 786-O cells Intraperitoneal injection 40 mg/kg Every two days for 7 weeks AZ505 significantly inhibited the growth of 786-O cell xenografts and reduced Ki67 expression Theranostics. 2019 Oct 22;9(26):8377-8391
Mice Pkd1nl/nl mouse model I.p. injection 5 mg/kg Daily from P7 to P27 AZ505 delayed cyst growth, as indicated by decreased cyst index, kidney weight to body weight ratio (KW/BW), and blood urea nitrogen (BUN) level; inhibited cystic epithelial cell proliferation; and induced cystic epithelial cell apoptosis. J Clin Invest. 2017 Jun 30;127(7):2751-2764

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.66mL

1.73mL

0.87mL

17.31mL

3.46mL

1.73mL

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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