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AV-412 free base

Chemical Structure : AV-412 free base

CAS No.: 451492-95-8

AV-412 free base (MP-412 free base;AV412 free base;AV 412 free base;MP412 free base;MP 412 free base)

Catalog No.: PC-42546Not For Human Use, Lab Use Only.

AV-412 free base (MP412) is a potent dual inhibitor of EGFR and ErbB2, inhibits EGFR/EGFR L858R/EGFR T790M/EGFR L858R, T790M/ErbB2 with IC50 of 1.5/0.5/0.8/2.3/19 nM respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AV-412 free base (MP412) is a potent dual inhibitor of EGFR and ErbB2, inhibits EGFR/EGFR L858R/EGFR T790M/EGFR L858R, T790M/ErbB2 with IC50 of 1.5/0.5/0.8/2.3/19 nM respectively.
AV-412 also inhibits Abl (IC50=41 nM), weakly inhibits Flt3 and Src.
AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM.
AV-412 inhibits EGF-dependent cell proliferation with IC50 of 100 nM; active in cancer xenograft models.

Physicochemical Properties

M.Wt 507.0022
Formula C27H28ClFN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO:≥ 50 mg/mL

Chemical Name/SMILES

2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-

References

1. Suzuki T, et al. Cancer Sci. 2007 Dec;98(12):1977-84.

2. Suzuki T, et al. Cancer Sci. 2009 Aug;100(8):1526-31.

3. Zhou Y, et al. Nat Biotechnol. 2010 Jan;28(1):71-8.

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