AV-412

SKU: orb1309962

Description

AV-412

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	451493-31-5
MW	851.41
Purity	99.92%
Formula	C₄₁H₄₄ClFN₆O₇S₂
SMILES	Cc1ccc(cc1)S(O)(=O)=O.Cc1ccc(cc1)S(O)(=O)=O.CN1CCN(CC1)C(C)(C)C#Cc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)C=C
Target	EGFR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.35 mM);DMSO:135 mg/mL (158.56 mM)

Bioactivity

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Target IC50	EGFR (T790M):0.79 nM\|EGFR (L858R):0.5 nM\|EGFR:0.75 nM\|ErbB2:19 nM\|EGFR (L858R/T790M):2.3 nM
In Vivo	In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth in A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed EGFR and ErbB2 autophosphorylation at doses corresponding to its antitumor efficacy. Various dosing schedules showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting frequent dosing is preferable. Additionally, MP-412 exhibited significant antitumor effects on the ErbB2-overexpressing KPL-4 breast cancer cell line, which is resistant to gefitinib. These studies indicate MP-412's potential as a therapeutic for cancers expressing EGFR and ErbB2, especially those resistant to first-generation small-molecule inhibitors. Read more...
In Vitro	In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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AV412, AV-412, AV 412, inhibit, Inhibitor, HER1, MP412, MP-412, MP 412, Epidermal growth factor receptor, ErbB-1, ErbB2, EGFRT790M, EGFRL858R, EGFRL858R/T790M, EGFR (T790M), EGFR (L858R), EGFR (L858R/T790M), EGFR

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Compound Identifiers

PubChem CID

11700696 ↗

Key Properties

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No computed properties available.

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AV-412 (orb1309962)

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CAS Number:	451492-95-8
MW:	507
Formula:	C₂₇H₂₈ClFN₆O

Purity:	>98% (HPLC)
CAS Number:	451493-31-5
MW:	851.41
Formula:	C₄₁H₄₄ClFN₆O₇S₂

AV-412

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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