AZD-5153( AZD5153 )

Catalog No. M12890 CAS No. 1869912-39-9

AZD-5153 is a potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM.

Purity : >98% (HPLC)

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Biological Information

Product Name

AZD-5153
Note

Research use only, not for human use.
Brief Description

AZD-5153 is a potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM.
Description

AZD-5153 is a potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM; simultaneously binds to two bromodomains in BRD4; exhibits antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.Blood Cancer Phase 1 Clinical.
In Vitro

——
In Vivo

——
Synonyms

AZD5153
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

Blood cancer

Chemical Information

CAS Number

1869912-39-9
Formula Weight

479.585
Molecular Formula

C25H33N7O3
Purity

>98% (HPLC)
Solubility

——
SMILES

CC1C(=O)N(CCN1CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5OC)C=C4)C
Chemical Name

(R)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Bradbury RH, et al. J Med Chem. 2016 Sep 8;59(17):7801-17. 2. Rhyasen GW, et al. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. 3. Collins TA, et al. CPT Pharmacometrics Syst Pharmacol. 2017 Jun;6(6):357-364.

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