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
ChemScene
Product number
CS-2402
Product name
AV-412freebase
Purity
98.07%
Packaging
10mg
Price
$180
Updated
2021/12/16
Activate Scientific
Product number
AS10021
Product name
AV-412
Purity
95+%
Packaging
1mg
Price
$237
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); EGFRL858R: 0.51 nM (IC50); EGFRL858R/T790M: 2.3 nM (IC50); EGFRT790M: 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

China 74 India 1 United Kingdom 2 United States 15 Global 92
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19552
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354;
Email
support@targetmol.com
Country
United States
ProdList
39035
Advantage
58
Aladdin Scientific
Tel
Email
tp@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
United States Biological
Tel
--
Fax
--
Email
sales@advtechind.com
Country
United States
ProdList
6075
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
AK Scientific, Inc.
Tel
--
Fax
--
Email
sales@aksci.com
Country
United States
ProdList
6347
Advantage
65
United States Biological
Tel
--
Fax
--
Email
chemicals@usbio.net
Country
United States
ProdList
6214
Advantage
80
Creative Enzymes
Tel
--
Fax
--
Email
info@creative-enzymes.com
Country
United States
ProdList
6057
Advantage
58
MedChemExpress
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58
Combi-Blocks Inc.
Tel
--
Fax
--
Email
sales@combi-blocks.com
Country
United States
ProdList
6618
Advantage
69
Matrix Scientific
Tel
--
Fax
--
Email
sales@matrixscientific.com
Country
United States
ProdList
6632
Advantage
80
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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