AZD6482 (S-isomer) | CAS#1173900-37-2 | 1173900-33-8 | PI3Kβ inhibitor

MedKoo Cat#: 406747 | Name: AZD6482 (S-isomer)

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). AZD6482 inhibited insulin-induced human adipocyte glucose uptake in vitro (IC(50) of 4.4 μm). This is the first human target validation for PI3Kβ inhibition as anti-platelet therapy showing a mild and generalized antiplatelet effect attenuating but not completely inhibiting multiple signaling pathways with an impressive separation towards primary hemostasis. AZD6482 at 'supratherapeutic' plasma concentrations may attenuate insulin signaling, most likely through PI3Kα inhibition.

Chemical Structure

AZD6482 (S-isomer)

CAS#1173900-37-2 (S-isomer)

Theoretical Analysis

MedKoo Cat#: 406747

Name: AZD6482 (S-isomer)

CAS#: 1173900-37-2 (S-isomer)

Chemical Formula: C22H24N4O4

Exact Mass: 408.1798

Molecular Weight: 408.46

Elemental Analysis: C, 64.69; H, 5.92; N, 13.72; O, 15.67

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,250.00	2 Weeks

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Related CAS #

1173900-33-8 (free base) 1173900-37-2 (S-isomer)

Synonym

AZD6482 (S-isomer); AZD6482 (S); AZD6482; AZD-6482; AZD 6482.

IUPAC/Chemical Name

(S)-2-((1-(7-methyl-2-morpholino-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethyl)amino)benzoic acid

InChi Key

IRTDIKMSKMREGO-HNNXBMFYSA-N

InChi Code

InChI=1S/C22H24N4O4/c1-14-11-17(15(2)23-18-6-4-3-5-16(18)22(28)29)21-24-19(12-20(27)26(21)13-14)25-7-9-30-10-8-25/h3-6,11-13,15,23H,7-10H2,1-2H3,(H,28,29)/t15-/m0/s1

SMILES Code

O=C(O)C1=CC=CC=C1N[C@H](C2=CC(C)=CN(C2=NC(N3CCOCC3)=C4)C4=O)C

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, not in water

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).

HS Tariff Code

2934.99.9001

More Info

Related: 1173900-37-2 (AZD6482 S-isomer) 1173900-33-8 (AZD6482)

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 408.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Wang J, Wen J, Yi R, Liu F, Zhou J, Liu G, Li Q, Yang Z, Su X. High selectivity of PI3Kβ inhibitors in SETD2-mutated renal clear cell carcinoma. J BUON. 2015 Sep-Oct;20(5):1267-75. PubMed PMID: 26537074. 2: Nylander S, Wågberg F, Andersson M, Skärby T, Gustafsson D. Exploration of efficacy and bleeding with combined phosphoinositide 3-kinase β inhibition and aspirin in man. J Thromb Haemost. 2015 Aug;13(8):1494-502. doi: 10.1111/jth.13027. Epub 2015 Jul 23. PubMed PMID: 26096765. 3: Cescon DW, Gorrini C, Mak TW. Breaking up is hard to do: PI3K isoforms on the rebound. Cancer Cell. 2015 Jan 12;27(1):5-7. doi: 10.1016/j.ccell.2014.12.003. PubMed PMID: 25584888. 4: Costa C, Ebi H, Martini M, Beausoleil SA, Faber AC, Jakubik CT, Huang A, Wang Y, Nishtala M, Hall B, Rikova K, Zhao J, Hirsch E, Benes CH, Engelman JA. Measurement of PIP3 levels reveals an unexpected role for p110β in early adaptive responses to p110α-specific inhibitors in luminal breast cancer. Cancer Cell. 2015 Jan 12;27(1):97-108. doi: 10.1016/j.ccell.2014.11.007. Epub 2014 Dec 24. PubMed PMID: 25544637; PubMed Central PMCID: PMC4745884. 5: Nichols AC, Black M, Yoo J, Pinto N, Fernandes A, Haibe-Kains B, Boutros PC, Barrett JW. Exploiting high-throughput cell line drug screening studies to identify candidate therapeutic agents in head and neck cancer. BMC Pharmacol Toxicol. 2014 Nov 27;15:66. doi: 10.1186/2050-6511-15-66. PubMed PMID: 25428177; PubMed Central PMCID: PMC4258049. 6: Laurent PA, Séverin S, Hechler B, Vanhaesebroeck B, Payrastre B, Gratacap MP. Platelet PI3Kβ and GSK3 regulate thrombus stability at a high shear rate. Blood. 2015 Jan 29;125(5):881-8. doi: 10.1182/blood-2014-07-588335. Epub 2014 Nov 14. PubMed PMID: 25398937. 7: Giordanetto F, Barlaam B, Berglund S, Edman K, Karlsson O, Lindberg J, Nylander S, Inghardt T. Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3936-43. doi: 10.1016/j.bmcl.2014.07.007. Epub 2014 Jul 9. PubMed PMID: 25042253. 8: Weigelt B, Warne PH, Lambros MB, Reis-Filho JS, Downward J. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44. doi: 10.1158/1078-0432.CCR-12-3815. Epub 2013 May 14. PubMed PMID: 23674493; PubMed Central PMCID: PMC3700760. 9: Jackson SP, Schoenwaelder SM. Antithrombotic phosphoinositide 3-kinase β inhibitors in humans: a 'shear' delight! J Thromb Haemost. 2012 Oct;10(10):2123-6. doi: 10.1111/j.1538-7836.2012.04912.x. PubMed PMID: 22943292. 10: Nylander S, Kull B, Björkman JA, Ulvinge JC, Oakes N, Emanuelsson BM, Andersson M, Skärby T, Inghardt T, Fjellström O, Gustafsson D. Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36. doi: 10.1111/j.1538-7836.2012.04898.x. PubMed PMID: 22906130.