Home Cart Sign in  
Chemical Structure| 153436-53-4 Chemical Structure| 153436-53-4

Structure of AG-1478
CAS No.: 153436-53-4

Chemical Structure| 153436-53-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

AG-1478 selectively inhibits EGFR with IC50 of 3 nM in cell-free assay.

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of AG-1478

CAS No. :153436-53-4
Formula : C16H14ClN3O2
M.W : 315.75
SMILES Code : COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC
MDL No. :MFCD00270914

Safety of AG-1478

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Related Pathways of AG-1478

RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
podocytes 500 nM 7 minutes HB-EGF induces apical protrusions in podocytes, which is blocked by AG1478. PMC3198052
podocytes 500 nM 8 hours HB-EGF increases podocyte migration, which is blocked by AG1478. PMC3198052
CAOV-3 cells 10 μM 72 hours AG1478 inhibited the proliferation of CAOV-3 cells, and the combination with WEB2086 showed synergistic effects with a CI value of 0.49 PMC4028110
SKOV-3 cells 10 μM 72 hours AG1478 inhibited the proliferation of SKOV-3 cells, and the combination with WEB2086 showed synergistic effects with a CI value of 0.58 PMC4028110
PANC-1 10 μM 96 hours AG1478 inhibited the growth of PANC-1 cells and blocked the phosphorylation of EGFR Tyr1068. PMC3847497
BxPC3 10 μM 96 hours AG1478 inhibited the growth of BxPC3 cells and blocked the phosphorylation of EGFR Tyr1068. PMC3847497
MIA PaCa-2 10 μM 96 hours AG1478 inhibited the growth of MIA PaCa-2 cells and blocked the phosphorylation of EGFR Tyr1068. PMC3847497
MCF-7 cells 100 nmol/L 2 hours Inhibited HER-2 activity, PI4KIIα knockdown extended the effective time of AG1478 PMC4026421
MCF-7 cells 5 nmol/L 2 hours PI4KIIα knockdown reduced the effective dose of AG1478 PMC4026421
A549 cells 5 μmol/L PI4KIIα knockdown and AG1478 combined treatment significantly inhibited cell survival PMC4026421
MDA-MB-231 cells 5 μmol/L PI4KIIα knockdown and AG1478 combined treatment significantly inhibited cell survival PMC4026421
podocytes 30 nM 7 minutes To assess the effect of HB-EGF on podocyte migration, results showed that HB-EGF induced podocyte migration, and this effect was blocked by AG-1478. PMC3198052
A549 cells 5 μmol/L 48 hours Combined inhibition of PI4KII α and EGFR was more effective in inhibiting cell viability PMC4026421
MDA-MB-231 cells 5 μmol/L 48 hours Combined inhibition of PI4KII α and EGFR was more effective in inhibiting cell viability PMC4026421

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice accelerated anti-GBM RPGN model intraperitoneal injection 5 mg/kg 24 hours and 1 hour before irradiation AG1478 significantly reduced crescentic lesions, albuminuria, and renal function impairment. PMC3198052
Nude mice CAOV-3 xenograft model Intraperitoneal injection 30 mg/kg twice daily for 4 days AG1478 inhibited the growth of CAOV-3 xenografts, and the combination with WEB2086 showed stronger antitumor effects PMC4028110
Mice cPLA 2α transgenic mice Intraperitoneal injection 10 mg/kg Every three days for 2 weeks Pretreatment with AG1478 exacerbated Jo2-mediated liver injury, as evidenced by increased hepatocyte apoptosis, elevated serum ALT and AST levels, and increased caspase-3, 8, 9 activities. PMC3221788
Nude mice Orthotopic pancreatic cancer model Intraperitoneal injection 3 mg/kg, 10 mg/kg, 30 mg/kg Twice daily, for 4 days Knockdown of STAT3 significantly reduced tumor burden and delayed tumor progression, increasing sensitivity to gemcitabine. PMC3847497
BALB/c nude mice MCF-7 cells induced xenografts oral 60 mg/kg once daily for 5 days PI4KIIα knockdown and Iressa combined treatment significantly inhibited tumor growth PMC4026421
mice anti-GBM glomerulonephritis model intraperitoneal injection 250 mg/kg BA, 10 mg/kg taxol BA every 2 days, taxol every 3 days, for 24 days To evaluate the inhibitory effect of AG-1478 on EGFR phosphorylation and its impact on glomerulonephritis, results showed that AG-1478 significantly reduced the severity of glomerular lesions and preserved renal function. PMC3198052
Mice cPLA 2α transgenic mice Intraperitoneal injection 10 mg/kg/day Every 2 days for 4 weeks To investigate the effect of AG1478 on Fas-induced liver injury, the results showed that AG1478 pretreatment significantly increased hepatocyte apoptosis and liver injury. PMC3221788
Nude mice CAOV-3 xenograft model Intraperitoneal injection 30 mg/kg/day once daily for 8 days To evaluate the antitumor effect of AG1478 alone or in combination with WEB2086 on CAOV-3 xenografts, the results showed that the combination significantly inhibited tumor growth. PMC4028110
BALB/c nude mice MCF-7 cell-induced xenografts oral 10 mg/kg Every three days for two weeks PI4KII α knockdown combined with Iressa treatment significantly inhibited tumor growth PMC4026421

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.84mL

3.17mL

1.58mL

31.67mL

6.33mL

3.17mL

References

 

Historical Records

Categories