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AZD5153

Cat. No. M9754
AZD5153 Structure
Synonym:

AZD-5153

Size Price Availability
10mg USD 550 1-2 Weeks
25mg USD 1100 1-2 Weeks
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM. AZD5153 could significantly disrupt BRD4 foci, with IC50 value of 1.7 nM in U2OS cells. AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19). 

In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 479.6
Formula C25H33N7O3
CAS Number 1869912-39-9
Purity >98%
Solubility DMSO ≥ 10 mg/mL
Storage at -20°C
References

AZD5153, a novel BRD4 inhibitor, suppresses human thyroid carcinoma cell growth in vitro and in vivo
Kun Xu, et al. Biochem Biophys Res Commun. 2018 May 15;499(3):531-537. PMID: 29596834.

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies
Garrett W Rhyasen, et al. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. PMID: 27573426.

Related Epigenetic Reader Domain Products
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MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively.

FL-411

FL-411 is a selective BRD4 inhibitor.

dBET6

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM.

dBET1

dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM.

ABBV-744

ABBV-744 is a BDII-selective BET bromodomain inhibitor that is used in the research of AML and metastic castration-resistant prostate cancer.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD5153, AZD-5153 supplier, Epigenetic Reader Domain, inhibitors

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