2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2) manufacturers
- AV-412
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- $37.00 / 1mg
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2025-11-10
- CAS:451493-31-5
- Min. Order:
- Purity: 99.92%
- Supply Ability: 10g
- AV-412
-
- $37.00 / 1mg
-
2025-11-10
- CAS:451493-31-5
- Min. Order:
- Purity: 99.92%
- Supply Ability: 10g
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| | 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2) Basic information |
| | 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:21.5(Max Conc. mg/mL);25.29(Max Conc. mM) DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.29(Max Conc. mM) DMF:15.0(Max Conc. mg/mL);17.64(Max Conc. mM) Ethanol:0.25(Max Conc. mg/mL);0.29(Max Conc. mM) | | form | Powder | | color | Light yellow to green yellow |
| | 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2) Usage And Synthesis |
| Uses | AV 412 is EGFR/HER2 inhibitor. It can be used in pharmacological activity and biological study of light-??assisted small-??molecule screening against protein kinases. | | Biological Activity | AV-412 (MP412) is an EGFR inhibitor with IC50 values of 0.75, 0.5, 0.79, 2.3 and 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. | | in vitro | AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC 50 of 43 and 282 nM, respectively. It also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC 50 of 100 nM. It abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. | | in vivo | In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. | | target | | EGFR 0.75 nM (IC 50 ) | EGFR L858R 0.5 nM (IC 50 ) | EGFR T790M 0.79 nM (IC 50 ) | EGFR < sup> L858R/T790M 2.3 nM (IC 50 ) | ErbB2 19 nM (IC 50 ) | | | IC 50 | EGFR: 0.75 nM (IC50); EGFRL858R: 0.5 nM (IC50); EGFRT790M: 0.79 nM (IC50); EGFRL858R/T790M: 2.3 nM (IC50); ErbB2: 19 nM (IC50) |
| | 2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-Methylbenzenesulfonate (1:2) Preparation Products And Raw materials |
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