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Ipatasertib
$50 – $2,600
Products Details
Product Description
– Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2].
Web ID
– HY-15186
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C24H32ClN5O2
Citations
– Biochem Pharmacol. 2020 Oct;180:114145.|Biomed Chromatogr. 2020 Oct;34(10):e4920.|Biomed Chromatogr. 2020 Oct;34(10):e4923.|Blood. 2023 May 26;blood.2022018752.|Cancer Immunol Immunother. 2020 Nov;69(11):2259-2273.|Cancer Res. 2021 Mar 8;canres.3232.2020.|Cancers (Basel). 2023 Nov 14, 15(22), 5407.|Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.|Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140.|Department of Laboratory Medicine, Laboratory of Hematology of the Radboudumc and Radboud Institute for Molecular Life Sciences in Nijmegen, The Netherlands.2019 Oct.|Elife. 2020 Dec 7;9:e61405.|EMBO Rep. 2020 Mar 4;21(3):e49129.|Haematologica. 2020 Mar;105(3):661-673.|Harvard Medical School LINCS LIBRARY|Int J Cancer. 2021 Apr 12.|Life Sci. 2020 Sep 1;256:117955.|Life Sci. 2021 Apr 19;277:119520.|Oncoimmunology. 2018 Aug 6;7(10):e1488565. |Oncol Rep. 2018 Aug;40(2):635-646. |Oncotarget. 2016 May 17;7(20):29131-42. |Oncotargets Ther. 2020 Aug 18;13:8197-8208.|Oxid Med Cell Longev. 2021 Jan 12;2021:3010548.|Patent. US20220313694A1.|Sci Adv. 2023 Mar 22;9(12):eadd5028.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Skelet Muscle. 2021 Mar 15;11(1):6.|SSRN. 2023 Jun 20.|Cell Rep. 2021 Feb 16;34(7):108744.|Mol Cell. 2020 Sep 17;79(6):1008-1023.e4.|Mol Cell. 2019 Jan 3;73(1):22-35.e6.
References
– [1]Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911.|[2]Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
CAS Number
– 1001264-89-6
Molecular Weight
– 458.00
Compound Purity
– 99.88
SMILES
– ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1
Clinical Information
– Phase 4
Research Area
– Cancer
Solubility
– DMSO : 220 mg/mL (ultrasonic)|H2O : 3.57 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Akt;Apoptosis
Isoform
– Akt1;Akt2;Akt3
Pathway
– Apoptosis;PI3K/Akt/mTOR
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
