AZD-5153 HNT salt
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MedKoo CAT#: 407809

CAS#: 1869912-40-2 (HNT salt)

Description: AZD-5153 HNT salt, is a 6-hydroxy-2-naphthoic acid salt of AZD-5153. AZD 5153 a potetn and selective orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). AZD5153 is highly Active against Hematologic Malignancies.


Price and Availability

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100mg
USD 1650
1g
USD 3850
Size
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200mg
USD 2250
2g
USD 5950
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500mg
USD 2950
5g
Ask price

AZD-5153 HNT salt, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407809
Name: AZD-5153 HNT salt
CAS#: 1869912-40-2 (HNT salt)
Chemical Formula: C36H41N7O6
Exact Mass:
Molecular Weight: 667.767
Elemental Analysis: C, 64.75; H, 6.19; N, 14.68; O, 14.38


Related CAS #: 1869912-39-9 (free base)   1869912-40-2 (HNT salt)    

Synonym: AZD-5153; AZD5153; AZD 5153; AZD-5153 6-hydroxy-2-naphthoate. AZD-5153 HNT salt.

IUPAC/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 6-hydroxy-2-naphthoate

InChi Key: UNZQBHXKCHECEC-GMUIIQOCSA-N

InChi Code: InChI=1S/C25H33N7O3.C11H8O3/c1-18-24(33)29(2)14-15-30(18)16-17-35-21-6-4-19(5-7-21)20-10-12-31(13-11-20)23-9-8-22-26-27-25(34-3)32(22)28-23;12-10-4-3-7-5-9(11(13)14)2-1-8(7)6-10/h4-9,18,20H,10-17H2,1-3H3;1-6,12H,(H,13,14)/t18-;/m1./s1

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


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Collins TA, Hattersley MM, Yates J, Clark E, Mondal M, Mettetal JT. Translational Modeling of Drug-Induced Myelosuppression and Effect of Pretreatment Myelosuppression for AZD5153, a Selective BRD4 Inhibitor. CPT Pharmacometrics Syst Pharmacol. 2017 Jun;6(6):357-364. doi: 10.1002/psp4.12194. Epub 2017 May 27. PubMed PMID: 28378926; PubMed Central PMCID: PMC5488126.

2: Yeh TC, O'Connor G, Petteruti P, Dulak A, Hattersley M, Barrett JC, Chen H. Identification of CCR2 and CD180 as Robust Pharmacodynamic Tumor and Blood Biomarkers for Clinical Use with BRD4/BET Inhibitors. Clin Cancer Res. 2017 Feb 15;23(4):1025-1035. doi: 10.1158/1078-0432.CCR-16-1658. Epub 2017 Jan 10. PubMed PMID: 28073847.

3: Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. Epub 2016 Aug 29. PubMed PMID: 27573426.

4: Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phen oxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153). J Med Chem. 2016 Sep 8;59(17):7801-17. doi: 10.1021/acs.jmedchem.6b00070. Epub 2016 Aug 24. PubMed PMID: 27528113.