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PI3K&mTOR

A66 (1166227-08-2)

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

Not Intended for Therapeutic Use. For research use only.

CAS: 1166227-08-2 Category

A66 (1166227-08-2) Description

A66 is a inhibitor of p110α P13K that exhibits anticaner chemotherapeutic activity.  P110a is the catalytic subunit of a class I Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic that is composed of a 85 kDa regulatory subunit and a 110 kDa catalytic subunit. A66 is more than 100 fold less active against the other class-I PI 3-kinase isoforms and had not inhibitory activity against 200 protein kinases when tested at 10 micromolar. This makes it the most selective and specific p110alpha inhibitor available for research purposes. A66 decreases cell viability of endometrial cancer cells and inhibits tumor growth of xenografts when administered in combination with other therapies. In animal models, A66 increases glucose output and impairs glucose and insulin tolerance.

A66 (1166227-08-2) Specification

Product Name A66
Synonym
Chemical Name (2S)-N1-[2-(1,1-Dimethylethyl)-4′-methyl[4,5′-bithiazol]-2′-yl]-1,2-pyrrolidinedicarboxamide,A-66, A 66, J-501023, CHEMBL3218581, AOB2329,CCT128930,  MLS006010983, (2S)-1-N-[5-(2-tert-Butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
Classification Biochemical, Chemical
Purity ≥98% (HPLC)
CAS Number 1166227-08-2
Molecular Formula C17H23N5O2S2
Molecular Weight 393.53
Monoisotopic Mass 393.129 g/mol
MDL number MFCD22378485
InChIKey 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 CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CSC(=N3)C(C)(C)C
Form Powder
Color white to beige
Solubility  DMSO: 20 mg/mL, clear; not in water
Storage Temp.  −20°C
Shelf life >2 years if stored properly
Handling Protect from air and light
Application An inhibitor for oncogenic forms of p110

 


RIDADR NONH for all modes of transport

References:

  • [1]. Park, Ga Bin; Kim, Daejin – Molecular and Cellular Biochemistry 2018 vol. 439 # 1-2 p. 199 – 211
  • [2]. Choi, Jae-Hyeog; Kim, Ki Hyang; Roh, Kug-Hwan; Jung, Hana; Lee, Anbok; Lee, Ji-Young; Song, Joo Yeon; (…) Yea, Sung Su; Park, SaeGwang – OncoImmunology 2018 vol. 7 # 5
  • [3]. Yang, Tao; Meoli, David F.; Moslehi, Javid; Roden, Dan M. – Journal of Pharmacology and Experimental Therapeutics 2018 vol. 365 # 3 p. 460 – 466