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Afuresertib - CAS 1047644-62-1

Inquiry

Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

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Molecular Formula

C18H17Cl2FN4OS

Molecular Weight

427.32

Afuresertib

- Specification
  - Related CAS
    
    1047645-82-8 (hydrochloride)
    
    Appearance
    
    Solid powder
    
    Synonyms
    
    GSK-2110183; GSK 2110183; GSK2110183; GSK-2110183B; GSK 2110183B; GSK2110183B; Afuresertib.
- Properties
  - InChI Key
    
    AFJRDFWMXUECEW-LBPRGKRZSA-N
    
    InChI
    
    InChI=1S/C18H17Cl2FN4OS/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26)/t12-/m0/s1
    
    Canonical SMILES
    
    CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl
- Reference Reading
  - 1.The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma.
    
    Spencer A1, Yoon SS2, Harrison SJ3, Morris SR4, Smith DA4, Brigandi RA5, Gauvin J4, Kumar R5, Opalinska JB5, Chen C6. Blood. 2014 Oct 2;124(14):2190-5. doi: 10.1182/blood-2014-03-559963. Epub 2014 Jul 29.
    
    The PI3K/AKT pathway is constitutively active in hematologic malignancies, providing proliferative and antiapoptotic signals and possibly contributing to drug resistance. We conducted an open-label phase 1 study to evaluate the maximum tolerated dose (MTD), safety, pharmacokinetics, and clinical activity of afuresertib-an oral AKT inhibitor-in patients with advanced hematologic malignancies. Seventy-three patients were treated at doses ranging from 25 to 150 mg per day. The MTD was established at 125 mg per day because of 2 dose-limiting toxicities in the 150-mg cohort (liver function test abnormalities). The most frequent adverse events were nausea (35.6%), diarrhea (32.9%), and dyspepsia (24.7%). Maximum plasma concentrations and area under the plasma concentration-time curves from time 0 to 24 hours were generally dose proportional at > 75-mg doses; the median time to peak plasma concentrations was 1.5 to 2.5 hours post dose, with a half-life of approximately 1.
    
    2.Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma.
    
    Tolcher AW1, Patnaik A, Papadopoulos KP, Rasco DW, Becerra CR, Allred AJ, Orford K, Aktan G, Ferron-Brady G, Ibrahim N, Gauvin J, Motwani M, Cornfeld M. Cancer Chemother Pharmacol. 2015 Jan;75(1):183-9. doi: 10.1007/s00280-014-2615-5. Epub 2014 Nov 25.
    
    PURPOSE: To identify the maximum tolerated dose (MTD) and recommended Phase II dose of MEK/AKT inhibitor combination of trametinib and afuresertib.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 2.3402 mL 11.7008 mL 23.4017 mL
    
    5 mM 0.4680 mL 2.3402 mL 4.6803 mL
    
    10 mM 0.2340 mL 1.1701 mL 2.3402 mL
    
    50 mM 0.0468 mL 0.2340 mL 0.4680 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.3402 mL	11.7008 mL	23.4017 mL
5 mM	0.4680 mL	2.3402 mL	4.6803 mL
10 mM	0.2340 mL	1.1701 mL	2.3402 mL
50 mM	0.0468 mL	0.2340 mL	0.4680 mL

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