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| Size | Price | Stock |
|---|---|---|
| 5mg | $145 | 3-6 Days |
| 10mg | $230 | 3-6 Days |
| 25mg | $385 | 3-6 Days |
| 50mg | $570 | 3-6 Days |
| 100mg | $855 | 3-6 Days |
| 250mg | $1450 | 3-6 Days |
| 500mg | $2080 | 3-6 Days |
: Cat #: V3824 CAS #: 1869912-39-9 Purity ≥ 98%
Description: AZD-5153 (AZD5153) is a potent, selective, and orally bioavailable BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with anticancer activity. It inhibits BRD4 with a pKi of 8.3 and possesses a bivalent binding mode. Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nmol/L. AZD5153 efficiently downregulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153. AML, MM, and DLBCL cell lines are highly sensitive to AZD5153. This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies.
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| Molecular Weight (MW) | 479.59 |
|---|---|
| Molecular Formula | C25H33N7O3 |
| CAS No. | 1869912-39-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (149.75 mM) |
| Water: <1 mg/mL | |
| Ethanol: 27 mg/mL warmed (40.43 mM) | |
| Synonyms | AZD-5153; AZD5153; AZD 5153. |
| Protocol | In Vitro | In vitro activity: Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nmol/L. AZD5153 efficiently downregulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153. AML, MM, and DLBCL cell lines are highly sensitive to AZD5153. Kinase Assay: AZD-5153 HNT salt, the 6-Hydroxy-2-naphthoic acid salt form of AZD5153, is a potent, selective, and orally available BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with pKi of 8.3 for BRD4 and possesses a bivalent binding mode. Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153. Cell Assay: Apoptosis was analyzed by flow cytometry using CellEvent Caspase 3/7 Green detection reagent. MV-4-11, MM.1S, and K562 cells were pretreated with AZD5153 or I-BET762 for 48 hours in culture media. Cells were collected and stained with 5 μmol/L final concentration of CellEvent for 30 minutes at 37°C. Flow cytometry was done on a BD Fortessa using the Blue laser and FITC filter set. |
|---|---|---|
| In Vivo | In vivo administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 modulates MYC and HEXIM1 in AML xenograft tumors and human whole blood. AZD5153 is administered orally to mice bearing MV-4-11 xenografts, and pharmacodynamic activity (intratumoral levels of c-Myc) is measured at 2, 4, and 8 h postdose. A considerable decrease in c-Myc expression is observed out to 8 h post dose at free plasma levels of compound<0.2 μM. This decrease in c-Myc expression after treatment with AZD5153 is consistent with other published BET inhibitors | |
| Animal model | Female CB17 SCID and SCID beige mice |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0851 mL | 10.4256 mL | 20.8511 mL | 41.7023 mL |
| 5mM | 0.4170 mL | 2.0851 mL | 4.1702 mL | 8.3405 mL |
| 10mM | 0.2085 mL | 1.0426 mL | 2.0851 mL | 4.1702 mL |
| 20mM | 0.1043 mL | 0.5213 mL | 1.0426 mL | 2.0851 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.