AZD 5153
Catalog No.
C3076
orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4.
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AZD5153 (CAS 1869912-39-9) is a potent, selective, orally bioavailable inhibitor of the bromodomain and extraterminal (BET) family protein BRD4. Through simultaneous binding of both bromodomains in BRD4, AZD5153 effectively disrupts BRD4-mediated transcriptional regulation. In cellular assays, AZD5153 demonstrates high activity, notably displacing BRD4 with an IC50 of approximately 1.7 nM in U2OS cells. It significantly inhibits growth of AML, multiple myeloma, and diffuse large B-cell lymphoma cell lines, reducing mTOR pathway signaling. In vivo, AZD5153 shows dose-dependent antitumor efficacy in xenograft models of hematologic malignancies, indicating its value as a tool compound in cancer research.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 479.6 |
| Cas No. | 1869912-39-9 |
| Formula | C25H33N7O3 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | (3R)-4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone |
| SDF | Download SDF |
| Canonical SMILES | COC1=NN=C2N1N=C(N3CCC(C4=CC=C(OCCN5[C@H](C)C(N(C)CC5)=O)C=C4)CC3)C=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
