Afuresertib hydrochloride

CAS No. 1047645-82-8

Afuresertib hydrochloride( GSK 2110183 hydrochloride | GSK2110183 hydrochloride )

Catalog No. M10235 CAS No. 1047645-82-8

A potent, selective, ATP-competitive pan-AKT inhibitor with biochemical IC50 of 0.08/2/2.6 nM for AKT1/2/3.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 40 Get Quote
5MG 61 Get Quote
10MG 86 Get Quote
25MG 149 Get Quote
50MG 239 Get Quote
100MG 414 Get Quote
200MG 538 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Afuresertib hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, ATP-competitive pan-AKT inhibitor with biochemical IC50 of 0.08/2/2.6 nM for AKT1/2/3.
  • Description
    A potent, selective, ATP-competitive pan-AKT inhibitor with biochemical IC50 of 0.08/2/2.6 nM for AKT1/2/3; also inhibits PKA (IC50=1.3 nM) and AKT1 E17K mutant (IC50=0.2 nM), selective over PKC, PKG isoforms and p70S6K; orally bioactive.Gastric Cancer Phase 1 Discontinued(In Vitro):Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase.Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response. (In Vivo):Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.
  • In Vitro
    Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.
  • In Vivo
    Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.
  • Synonyms
    GSK 2110183 hydrochloride | GSK2110183 hydrochloride
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    Akt
  • Recptor
    Akt
  • Research Area
    Cancer
  • Indication
    Gastric Cancer

Chemical Information

  • CAS Number
    1047645-82-8
  • Formula Weight
    463.7841
  • Molecular Formula
    C18H18Cl3FN4OS
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 52 mg/mL
  • SMILES
    CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl.Cl
  • Chemical Name
    2-Thiophenecarboxamide, N-[(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-, hydrochloride (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Dumble M, et al. PLoS One. 2014 Jun 30;9(6):e100880. 2. Spencer A, et al. Blood. 2014 Oct 2;124(14):2190-5. 3. Arceci RJ, et al. Pediatr Blood Cancer. 2017 May;64(5).
molnova catalog
related products
  • Methyl hesperidin

    Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits.

  • GSK-690693

    A potent, ATP competitive, pan-AKT inhibitor with IC50 of 2, 13, and 9 nM against AKT1, 2, and 3, respectively.

  • Lupeol

    Lupeol is a pentacyclic triterpene that has anti-inflammatory and antioxidant activity.