| Identification | Back Directory | [Name]
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) | [CAS]
451493-31-5 | [Synonyms]
MP-412;MP412
AV-412 / MP-412
AV-412 Tosylate
451492-95-8 (AV-412 FREE BASE)
MP-412;AV412;AV 412;MP412;MP 412
N-[4-(3-Chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide tosylate
N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide,4-methylbenzenesulfonic acid
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-quinazolinyl]-2-propenamide bis(4-methylbenzenesulfonate)
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) | [Molecular Formula]
C41H44ClFN6O7S2 | [MOL File]
451493-31-5.mol | [Molecular Weight]
851.405 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 ) | | [storage]
Store at -20°C |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|