ChemicalBook > CAS DataBase List > MP-412

MP-412

Product Name: MP-412
CAS No.: 451492-95-8
Chemical Name: MP-412
Synonyms: MP-412;AV-412;CS-2307;MP-412 free base;AV-412 (free base);AV-412 free base/451492-95-8;AV 412 free base,AV412 free base;AV-412 free base (MP-412 free base);AV-412;MP-412;AV 412;MP 412;AV412;MP412;N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quin
CBNumber: CB52500949
Molecular Formula: C27H28ClFN6O
Formula Weight: 507
MOL File: 451492-95-8.mol

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MP-412 Property

Boiling point:: 672.9±55.0 °C(Predicted)
Density: 1.33
storage temp.: Store at -20°C
solubility: DMSO: ≥ 50 mg/mL (98.62 mM)
pka: 11.61±0.43(Predicted)
form: Powder
color: White to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Tocris

Product number: 4397
Product name: AV412
Purity: ≥98%(HPLC)
Packaging: 10
Price: $228
Updated: 2021/12/16

TRC

Product number: A794728
Product name: AV412
Packaging: 1mg
Price: $45
Updated: 2021/12/16

ChemScene

Product number: CS-2402
Product name: AV-412freebase
Purity: 98.07%
Packaging: 5mg
Price: $108
Updated: 2021/12/16

Activate Scientific

Product number: AS10021
Product name: AV-412
Purity: 95+%
Packaging: 1mg
Price: $237
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: KIN0000412
Product name: AV-412
Purity: 95.00%
Packaging: 1MG
Price: $340.2
Updated: 2021/12/16

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MP-412 Chemical Properties,Usage,Production

Uses

AV 412 is used in the synthetic preparation of phenylaminoquinazoline derivatives as inhibitors of tyrosine-specific protein kinase for preparation and/or treatment of cancers, diseases caused by arteriosclerosis, or psoriasis.

Synthesis

451494-30-7

79-10-7

451492-95-8

Amino compound 2a (6.08 g, 13.4 mmol), acrylic acid (1.38 mL, 20.1 mmol), triethylamine (2.8 mL, 20.1 mmol) and EDC (3.86 g, 20.1 mmol) were dissolved in DMF (100 mL) and the reaction was stirred at room temperature overnight. Subsequently, acrylic acid (0.46 mL, 6.71 mmol), triethylamine (0.93 mL, 6.71 mmol) and EDC (1.29 g, 6.71 mmol) were added to the reaction system and the reaction was continued with stirring overnight. Upon completion of the reaction, the mixture was poured into aqueous sodium bicarbonate (300 mL) and the precipitate was collected by filtration. The precipitate was washed sequentially with water and ethanol-water solvent mixture and dried. The crude product was dissolved in ethanol-water mixed solvent by heating and stirring, cooled to room temperature and filtered, and the precipitate was collected and dried to afford the target product N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide 1a (3.41 g, 50% yield). [CHEMMOL-00368] 1H NMR (DMSO-d6) δ ppm of 1a: 1.44 (s, 6H), 2.15 (s, 3H), 2.35 (br s, 4H), 2.64 (br s, 4H), 5.85 (d, J = 10.3 Hz, 1H), 6.33 (d, J = 16.9 Hz, 1H), 6.58 ( dd, J = 10.3,16.9 Hz, 1H), 7.47 (t, J = 9.1 Hz, 1H), 7.84 (br s, 2H), 8.20 (br d, J = 6.1 Hz, 1H), 8.64 (s, 1H), 8.69 (s, 1H), 9.88 (s, 1H), 10.01 (s, 1H).

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^[1].

IC 50

EGFR: 0.75 nM (IC₅₀); ErbB2: 19 nM (IC₅₀); EGFR^L858R: 0.51 nM (IC₅₀); EGFR^L858R/T790M: 2.3 nM (IC₅₀); EGFR^T790M: 0.79 nM (IC₅₀)

References

[1] Patent: US2004/116422, 2004, A1. Location in patent: Page/Page column 32-33

MP-412 Preparation Products And Raw materials

Raw materials

Preparation Products

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MP-412 Suppliers

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View Lastest Price from MP-412 manufacturers

Career Henan Chemical Co

Product: N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide 451492-95-8
Price: US $1.00/KG
Min. Order: 1g
Purity: Min98% HPLC
Supply Ability: g/kg /ton
Release date: 2019-12-20

451492-95-8, MP-412Related Search:

2-PropenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-Methyl-3-(4-Methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-

AV-412 (free base)

N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide

N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quin

AV-412

MP-412

N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide

AV-412 free base (MP-412 free base)

AV-412;MP-412;AV 412;MP 412;AV412;MP412

CS-2307

N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide

MP-412 free base

AV 412 free base,AV412 free base

AV-412 free base/451492-95-8

451492-95-8

C27H28ClFN6O