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AZD2461

Product Name
AZD2461
CAS No.
1174043-16-3
Chemical Name
AZD2461
Synonyms
CS-739;AZD2461;AZD2461 ，S7029;AZD 2461, >=98%;AZD2461 AZD-2461;AZD2461 USP/EP/BP;AZD-2461, 10 mM in DMSO;4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one;4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one;4-[[4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one
CBNumber
CB62655394
Molecular Formula
C22H22FN3O3
Formula Weight
395.43
MOL File
1174043-16-3.mol
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AZD2461 Property

Density 
1.33±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥45.2 mg/mL in EtOH with ultrasonic
form 
powder
pka
12.07±0.40(Predicted)
color 
white to beige
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P314Get medical advice/attention if you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1858
Product name
AZD2461
Purity
≥98% (HPLC)
Packaging
5MG
Price
$108
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1858
Product name
AZD2461
Purity
≥98% (HPLC)
Packaging
25MG
Price
$218
Updated
2025/07/31
Cayman Chemical
Product number
16876
Product name
AZD 2461
Purity
≥95%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
16876
Product name
AZD 2461
Purity
≥95%
Packaging
5mg
Price
$183
Updated
2024/03/01
Cayman Chemical
Product number
16876
Product name
AZD 2461
Purity
≥95%
Packaging
10mg
Price
$341
Updated
2024/03/01
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AZD2461 Chemical Properties,Usage,Production

Uses

4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one is a phthalazinone derivative and potential PARP inhibitor.

Biochem/physiol Actions

AZD2461, an olaparib analog, is an orally available, potent and selective PARP1 and PARP2 inhibitor that is a poor substrate for drug transporters. AZD2461 exhibits a high efficacy in olaparib-resistant tumors that overexpress P-glycoprotein.

Synthesis

763114-26-7

4045-25-4

1174043-16-3

Example 1; 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (231 g, 1.206 mol) was added to a solution of dichloromethane (4.7 g, 0.251 mol) containing 4-methoxypiperidine hydrochloride (183 g, 1.206 mol), 5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoic acid (300 g, 1.005 mol), and 4-dimethylamino pyridine (30.7 g, 0.251 mol) in a solution of dichloromethane (4 L) was reacted at 23 °C. The resulting suspension was stirred at room temperature overnight. The reaction mixture was washed sequentially with 2 M hydrochloric acid (5 L) and 50% saturated sodium carbonate solution (3 L), followed by drying with anhydrous magnesium sulfate, filtration and concentration in vacuo to give the crude product. The crude product was slurried in ethyl acetate (750 mL) for 5 days, filtered and dried at 45 °C for 5 h to afford 4-[4-fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one (Compound 1) (290 g, 72.9% yield).1H NMR (400.132 MHz, DMSO) δ 1.26-1.35 ( 1H, m), 1.40-1.49 (1H, m), 1.69-1.73 (1H, m), 1.84-1.89 (1H, m), 2.99-3.07 (1H, m), 3.25 (3H, s), 3.27-3.34 (2H, m), 3.39-3.44 (1H, m), 3.86-3.95 (1H, m), 4.33 (2H, s). 4.33 (2H, s), 7.19-7.24 (1H, m), 7.33-7.35 (1H, m), 7.39-7.43 (1H, m), 7.81-7.91 (2H, m), 7.97 (1H, d), 8.27 (1H, d), 12.57 (1H, s); m/z (ES+) (M + H)+ = 396.31 ; HPLC tR = 1.90 min. Figure 1 illustrates the powder XRD pattern of the product showing it in crystalline form. Figure 2 illustrates the DSC analysis of the product.

in vivo

AZD-2461 (10 mg/kg, p.o.) enhances the antitumor activity of temozolomide in a mouse colorectal xenograft and exhibits low effect on mouse bone marrow cells. However, the increased bone marrow tolerability of AZD-2461 is not seen in rat models[1]. AZD-2461 (0.5% v/w HPMC, p.o.) increases the survival of mice bearing KB1P tumors after short-term treatment, and long-term treatment is well tolerated, but can not lead to tumor eradication[3].

IC 50

PARP2: 2 nM (IC50); PARP1: 5 nM (IC50); PARP3: 200 nM (IC50)

storage

Store at -20°C

References

[1] Patent: US2011/15393, 2011, A1. Location in patent: Page/Page column 7

AZD2461 Preparation Products And Raw materials

Raw materials

Preparation Products

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AZD2461 Suppliers

Canada 1 China 110 India 2 United Kingdom 1 United States 16 Global 130
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
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55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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76
Beijing HwrkChemical Technology Co., Ltd
Tel
18515581800 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
9400
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55
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
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65
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
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58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
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61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
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AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
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ApexBio Technology LLC
Tel
+1-832-696-8203
Fax
+1-832-641-3177
Email
info@apexbt.com
Country
United States
ProdList
477
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TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
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View Lastest Price from AZD2461 manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
AZD2461 1174043-16-3
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1Ton
Release date
2022-10-13
Career Henan Chemical Co
Product
AZD2461 1174043-16-3
Price
US $3.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
100KG
Release date
2020-01-29

1174043-16-3, AZD2461Related Search:

FLURBIPROFEN AXETIL Nintedanib SB525334 Veliparib Rapamycin PLX4032 Olaparib

  • 4-[[4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one
  • 4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
  • CS-739
  • AZD2461
  • 4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one
  • 1(2H)-Phthalazinone, 4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-
  • AZD 2461, >=98%
  • AZD2461 USP/EP/BP
  • 4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one
  • AZD2461 AZD-2461
  • AZD-2461, 10 mM in DMSO
  • AZD2461 ，S7029
  • 1174043-16-3
  • Inhibitors
  • Inhibitor