AZD5153 HNT salt
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1900 | Check With Us |
500mg | $2800 | Check With Us |
1g | $4200 | Check With Us |
Cat #: V2765 CAS #: 1869912-40-2 Purity ≥ 98%
Description: 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.
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Molecular Weight (MW) | 667.75 |
---|---|
Molecular Formula | C25H33N7O3.C11H8O3 |
CAS No. | 1869912-40-2 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 100 mg/mL (149.75 mM)r |
Water: <1 mg/mLr | |
Ethanol: 27 mg/mL warmed (40.43 mM) | |
SMILES Code | O=C1N(C)CCN(CCOC2=CC=C(C3CCN(C4=NN5C(C=C4)=NN=C5OC)CC3)C=C2)[C@@H]1C.O=C(O)C6=CC=C7C=C(O)C=CC7=C6 |
Synonyms | AZD5153; AZD 5153; AZD-5153 6-Hydroxy-2-naphthoic acid; AZD-5153; AZD-5153 6-hydroxy-2-naphthoate. AZD-5153 HNT salt. |
Protocol | In Vitro | AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153. |
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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 treatment markedly impacts transcriptional programs of MYC, E2F, and mTOR. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.4976 mL | 7.4878 mL | 14.9757 mL | 29.9513 mL |
5mM | 0.2995 mL | 1.4976 mL | 2.9951 mL | 5.9903 mL |
10mM | 0.1498 mL | 0.7488 mL | 1.4976 mL | 2.9951 mL |
20mM | 0.0749 mL | 0.3744 mL | 0.7488 mL | 1.4976 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.