AZD8186
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406260

CAS#: 1627494-13-6

Description: AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity. Upon administration, PI3Kbeta inhibitor AZD8186 selectively inhibits the activity of PI3Kbeta in the PI3K/Akt/mTOR signaling pathway, which may result in a decrease of tumor cell proliferation. It also induces cell death in PI3K-expressing cancer cells. By specifically targeting class I PI3K beta, this agent may be more efficacious and less toxic than pan PI3K inhibitors. PI3K-mediated signaling is often dysregulated in cancer cells and contributes to increased tumor cell growth, survival, and tumor resistance to a variety of antineoplastic agents. AZD8186 is currently under Phase I clinical trials.


Chemical Structure

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AZD8186
CAS# 1627494-13-6

Theoretical Analysis

MedKoo Cat#: 406260
Name: AZD8186
CAS#: 1627494-13-6
Chemical Formula: C24H25F2N3O4
Exact Mass: 457.18131
Molecular Weight: 457.4
Elemental Analysis: C, 63.01; H, 5.51; F, 8.31; N, 9.19; O, 13.99

Size Price Shipping out time Quantity
10mg USD 150 Same Day
25mg USD 250 Same Day
50mg USD 450 Same Day
100mg USD 850 Same Day
200mg USD 1250 Same Day
500mg USD 1950 Same Day
1g USD 2950 Same Day
2g USD 4650 Same Day
5g USD 7450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-04. Prices are subject to change without notice.

AZD-8186 purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: AZD8186; AZD 8186; AZD-8186.

IUPAC/Chemical Name: (R)-8-(1-((3,5-difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide

InChi Key: LMJFJIDLEAWOQJ-CQSZACIVSA-N

InChi Code: InChI=1S/C24H25F2N3O4/c1-14(27-18-11-16(25)10-17(26)12-18)19-8-15(24(31)28(2)3)9-20-21(30)13-22(33-23(19)20)29-4-6-32-7-5-29/h8-14,27H,4-7H2,1-3H3/t14-/m1/s1

SMILES Code: O=C(N(C)C)C1=CC([C@@H](C)NC2=CC(F)=CC(F)=C2)=C3C(C(C=C(O3)N4CCOCC4)=O)=C1

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

Preparing Stock Solutions

The following data is based on the product molecular weight 457.4 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-Van Der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Peru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N. Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chrom ene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. J Med Chem. 2014 Dec 16. [Epub ahead of print] PubMed PMID: 25514658.

2: Hancox U, Cosulich S, Hanson L, Trigwell C, Lenaghan C, Ellston R, Dry H, Crafter C, Barlaam B, Fitzek M, Smith PD, Ogilvie D, D'Cruz C, Castriotta L, Wedge SR, Ward L, Powell S, Lawson M, Davies BR, Harrington EA, Foster E, Cumberbatch M, Green S, Barry ST. Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN deficient breast and prostate tumour alone and in combination with docetaxel. Mol Cancer Ther. 2014 Nov 14. pii: molcanther.0406.2014. [Epub ahead of print] PubMed PMID: 25398829.

3: Marques RB, Aghai A, de Ridder CM, Stuurman D, Hoeben S, Boer A, Ellston RP, Barry ST, Davies BR, Trapman J, van Weerden WM. High Efficacy of Combination Therapy Using PI3K/AKT Inhibitors with Androgen Deprivation in Prostate Cancer Preclinical Models. Eur Urol. 2014 Sep 11. pii: S0302-2838(14)00806-9. doi: 10.1016/j.eururo.2014.08.053. [Epub ahead of print] PubMed PMID: 25220373.



Additional Information

AZD8186 is a novel potent small molecule that targets the lipid kinase PI3Kβ with selectivity vs PI3Kα. AZD8186 reduces pAKT-S473 in the PTEN deficient MDA-MB-468 cell line with an IC50 <5nM, while in the PI3Kα-dependent PIK3CA mutant line BT474 it is 200 fold less potent. AZD8186 also demonstrates cellular activity versus PI3Kβ, inhibiting IgM-dependent pAKT-S473 with an IC50 of 15nM.