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

AZD6482 (S-isomer)
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406747

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

Description: 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)

Instruction

Theoretical Analysis

MedKoo Cat#: 406747
Name: AZD6482 (S-isomer)
CAS#: 1173900-37-2 (S-isomer)
Chemical Formula: C22H24N4O4
Exact Mass: 408.18
Molecular Weight: 408.458
Elemental Analysis: C, 64.69; H, 5.92; N, 13.72; O, 15.67

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Biological target:
In vitro activity:
In vivo activity:

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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AZD6482 (S-isomer) featured