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); 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
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1077
Advantage
64
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
SYN|thesis med chem P/L
Tel
+86-021-50720296
Fax
+86-021-50720297
Email
service@synkinase.com
Country
China
ProdList
266
Advantage
58
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Nanjing Dulai Biotechnology Co., Ltd.
Tel
025-846993838003-8003 18013301590
Fax
025-84699383-8003
Email
njduly@126.com
Country
China
ProdList
3249
Advantage
55
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4768
Advantage
55
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9248
Advantage
55
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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