E7449

CAS No. 1140964-99-3

E7449( E-7449 | 2X-121 )

Catalog No. M10499 CAS No. 1140964-99-3

E7449 (2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 63 Get Quote
5MG 105 Get Quote
10MG 178 Get Quote
25MG 367 Get Quote
50MG 534 Get Quote
100MG 777 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    E7449
  • Note
    Research use only, not for human use.
  • Brief Description
    E7449 (2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2).
  • Description
    E7449 (2X-121) is a potent, orally bioavailable, brain penetrable dual inhibitor of PARP1/2 and TNKS1/2 with IC50 of 2.0/1.0 nM (PARP1/2), 50-100 nM (TNKS1/2); displays no significant inhibitory activity for PARP3 or PARPs6-16; shows sensitivity to cells deficient in DNA repair pathways beyond homologous recombination, inhibits Wnt/β-catenin signaling in colon cancer cell lines, stabilizes axin and TNKS proteins resulting in β-catenin de-stabilization and significantly alters expression of Wnt target genes; potentiates antitumor activity of chemotherapies temozolomide and carboplatin both in vitro and in vivo.Breast Cancer Phase 2 Clinical(In Vitro):Stenoparib is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ~50 and ~50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate. Stenoparib shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. Stenoparib traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). Stenoparib most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). Stenoparib (10 μM) inhibits Wnt signaling in SW480 cells. (In Vivo):Stenoparib moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model. Stenoparib (30 or 100 mg/kg, p.o.) inhibits PARP, shows anti-tumor activity, and is well-tolerated without any obvious body weight loss or deaths in a BRCA mutant xenograft model. Stenoparib (30, 100 or 300 mg/kg, p.o.) suppresses re-growth of hair in a dose dependent manner, and blocks Wnt signaling in C57BL/6 mice. Stenoparib (100 mg/kg, p.o.) combined with MEK inhibitor exhibits antitumor activity in a Wnt1 subcutaneous model (mammary tumors initially isolated from Wnt1 (int-1) transgenic mice).
  • In Vitro
    Stenoparib is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ~50 and ~50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate. Stenoparib shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. Stenoparib traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). Stenoparib most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). Stenoparib (10 μM) inhibits Wnt signaling in SW480 cells.
  • In Vivo
    Stenoparib moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model. Stenoparib (30 or 100 mg/kg, p.o.) inhibits PARP, shows anti-tumor activity, and is well-tolerated without any obvious body weight loss or deaths in a BRCA mutant xenograft model. Stenoparib (30, 100 or 300 mg/kg, p.o.) suppresses re-growth of hair in a dose dependent manner, and blocks Wnt signaling in C57BL/6 mice. Stenoparib (100 mg/kg, p.o.) combined with MEK inhibitor exhibits antitumor activity in a Wnt1 subcutaneous model (mammary tumors initially isolated from Wnt1 (int-1) transgenic mice).
  • Synonyms
    E-7449 | 2X-121
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    1140964-99-3
  • Formula Weight
    317.3446
  • Molecular Formula
    C18H15N5O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: < 6.96 mg/mL
  • SMILES
    O=C1NN=C(N2)C3=C(C=CC=C31)N=C2CN(C4)CC5=C4C=CC=C5
  • Chemical Name
    3H-Pyridazino[3,4,5-de]quinazolin-3-one, 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro-

Shipping & Storage Information

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

Reference

1. McGonigle S, et al. Oncotarget. 2015 Dec 1;6(38):41307-23. 2. Sharon McGonigle, et al. Abstract 4688: E7449: A novel PARP inhibitor enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors . Cancer Research: April 15, 2012; Volume 72, Issue 8, Su
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