A66
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MedKoo CAT#: 407127

CAS#: 1166227-08-2

Description: A66 is a potent and highly selective p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms. A66 blocks phosphoinositide 3-kinase signalling and tumour growth in certain cell types.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2250
Size
Price

25mg
USD 250
200mg
USD 850
2g
USD 3950
Size
Price

50mg
USD 450
500mg
USD 1250
5g
USD 6450

A66 purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 400mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407127
Name: A66
CAS#: 1166227-08-2
Chemical Formula: C17H23N5O2S2
Exact Mass: 393.12932
Molecular Weight: 393.52
Elemental Analysis: C, 51.89; H, 5.89; N, 17.80; O, 8.13; S, 16.29


Synonym: A66; A-66; A 66.

IUPAC/Chemical Name: (S)-N1-(2-(tert-butyl)-4'-methyl-[4,5'-bithiazol]-2'-yl)pyrrolidine-1,2-dicarboxamide

InChi Key: HBPXWEPKNBHKAX-NSHDSACASA-N

InChi Code: InChI=1S/C17H23N5O2S2/c1-9-12(10-8-25-14(20-10)17(2,3)4)26-15(19-9)21-16(24)22-7-5-6-11(22)13(18)23/h8,11H,5-7H2,1-4H3,(H2,18,23)(H,19,21,24)/t11-/m0/s1

SMILES Code: O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CSC(C(C)(C)C)=N3)S2


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


References

1: Sweetlove M, Wrightson E, Kolekar S, Rewcastle GW, Baguley BC, Shepherd PR, Jamieson SM. Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth. Front Oncol. 2015 Jun 16;5:135. doi: 10.3389/fonc.2015.00135. eCollection 2015. PubMed PMID: 26137449; PubMed Central PMCID: PMC4468830.

2: Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One. 2013 Sep 9;8(9):e73149. doi: 10.1371/journal.pone.0073149. eCollection 2013. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/70d3c7b0-9718-4bb1-abed-d0defc3b7fc4. PubMed PMID: 24039875; PubMed Central PMCID: PMC3767810.

3: Buchanan CM, Dickson JM, Lee WJ, Guthridge MA, Kendall JD, Shepherd PR. Oncogenic mutations of p110α isoform of PI 3-kinase upregulate its protein kinase activity. PLoS One. 2013 Aug 1;8(8):e71337. doi: 10.1371/journal.pone.0071337. Print 2013. PubMed PMID: 23936502; PubMed Central PMCID: PMC3731339.

4: Wang X, Li JP, Yang Y, Ding J, Meng LH. A pharmacological model reveals biased dependency on PI3K isoforms for tumor cell growth. Acta Pharmacol Sin. 2013 Sep;34(9):1201-7. doi: 10.1038/aps.2013.81. Epub 2013 Jul 29. PubMed PMID: 23892273; PubMed Central PMCID: PMC4003165.

5: Smith GC, Ong WK, Costa JL, Watson M, Cornish J, Grey A, Gamble GD, Dickinson M, Leung S, Rewcastle GW, Han W, Shepherd PR. Extended treatment with selective phosphatidylinositol 3-kinase and mTOR inhibitors has effects on metabolism, growth, behaviour and bone strength. FEBS J. 2013 Nov;280(21):5337-49. doi: 10.1111/febs.12428. Epub 2013 Aug 12. PubMed PMID: 23837532.

6: 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.

7: Smith GC, Ong WK, Rewcastle GW, Kendall JD, Han W, Shepherd PR. Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo. Biochem J. 2012 Feb 15;442(1):161-9. doi: 10.1042/BJ20111913. PubMed PMID: 22142257; PubMed Central PMCID: PMC3343648.

8: Jamieson S, Flanagan JU, Kolekar S, Buchanan C, Kendall JD, Lee WJ, Rewcastle GW, Denny WA, Singh R, Dickson J, Baguley BC, Shepherd PR. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J. 2011 Aug 15;438(1):53-62. doi: 10.1042/BJ20110502. PubMed PMID: 21668414; PubMed Central PMCID: PMC3174055.