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Size | Price | Stock |
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250mg | $945 | Check With Us |
500mg | $1450 | Check With Us |
1g | $2175 | Check With Us |
Cat #: V11916 CAS #: 451493-31-5 Purity ≥ 98%
Description: AV-412 Tosylate (also known as AV412; MP-412), the tosyulate salt of AV412, is a novel, 2nd generation and orally bioavailable EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
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- Protocol
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Molecular Weight (MW) | 851.41 |
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Molecular Formula | C41H44ClFN6O7S2 |
CAS No. | 451493-31-5 |
SMILES Code | CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CC(C)(C#CC1=CC2=C(C=C1NC(=O)C=C)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)N4CCN(CC4)C |
Synonyms | MP-412; MP 412; MP412; AV-412; AV 412; AV412; AV-412 tosylate |
Protocol | In Vitro | AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC50 of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
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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. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.1745 mL | 5.8726 mL | 11.7452 mL | 23.4904 mL |
5mM | 0.2349 mL | 1.1745 mL | 2.3490 mL | 4.6981 mL |
10mM | 0.1175 mL | 0.5873 mL | 1.1745 mL | 2.3490 mL |
20mM | 0.0587 mL | 0.2936 mL | 0.5873 mL | 1.1745 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.