ChemicalBook > CAS DataBase List > A-966492

A-966492

Product Name
A-966492
CAS No.
934162-61-5
Chemical Name
A-966492
Synonyms
CS-903;A-966492;A-966492, >=98%;A-966492 USP/EP/BP;A-966492(A 966492);A966492;A 966492;A-966492;A-966492 PARP inhibitor A966492;2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide;2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide;1H-Benzimidazole-7-carboxamide, 2-[2-fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-
CBNumber
CB42522977
Molecular Formula
C18H17FN4O
Formula Weight
324.35
MOL File
934162-61-5.mol
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A-966492 Property

Boiling point:
605.5±65.0 °C(Predicted)
Density 
1.335
storage temp. 
Store at -20°C
solubility 
≥32.4 mg/mL in DMSO; ≥16.53 mg/mL in H2O with ultrasonic; ≥3.16 mg/mL in EtOH with gentle warming and ultrasonic
form 
solid
pka
9.33±0.30(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
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N-Bromosuccinimide Price

Cayman Chemical
Product number
26378
Product name
A-966492
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
26378
Product name
A-966492
Packaging
25mg
Price
$533
Updated
2024/03/01
Cayman Chemical
Product number
26378
Product name
A-966492
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
26378
Product name
A-966492
Packaging
10mg
Price
$261
Updated
2024/03/01
ApexBio Technology
Product number
A4160
Product name
A-966492
Packaging
50mg
Price
$590
Updated
2021/12/16
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A-966492 Chemical Properties,Usage,Production

Uses

A-966492 effectively inhibits PARP-1 with an EC50 of 1 nM and a Ki value of 1 nM. When it acts on PARP-2, the Ki value is 1.5 nM. It has excellent efficacy on PARP enzyme, especially on C41 cells. A-966492 significantly enhanced the effect of TMZ in a dose-dependent manner.

Biological Activity

a-966492 is an inhibitor of parp-1 with ki value of 1nm [1].parp-1 belongs to the poly(adp-ribose) polymerases (parps) family, it contributes to the resistance happened after cancer therapy. a-966492 is a potent inhibitor of both parp-1 and parp-2 (ki value of 1.5nm) with good potency in c41 whole cells (ec50 value of 1nm). a-966492 shows excellent pharmaceutical properties with oral bioavailabilities of 34-72% and half-lives of 1.7-1.9 h. additionally, a-966492 can crosses the blood-brain barrier. a-966492 is proved potent in a murine b16f10 syngeneic melanoma model and a brca1-deficient mx-1 breast carcinoma model. meanwhile, it can enhance the efficacy of tmz and carboplatin in these models [1].

Synthesis

A-966492 is prepared by reacting 3-Carboxamido-1,2-phenylenediamine with benzoic acid in a solution(methanol:water=1:1) at 50 °C for 2 hours.

References

[1] penning td, zhu gd, gong j, thomas s, gandhi vb, liu x, shi y, klinghofer v, johnson ef, park ch, fry eh, donawho ck, frost dj, buchanan fg, bukofzer gt, rodriguez le, bontcheva-diaz v, bouska jj, osterling dj, olson am, marsh kc, luo y, giranda vl. optimization of phenyl-substituted benzimidazole carboxamide poly(adp-ribose) polymerase inhibitors: identification of (s)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1h-benzimidazole-4-carboxamide (a-966492), a highly potent and efficacious inhibitor. j med chem. 2010 apr 22;53(8):3142-53.

A-966492 Preparation Products And Raw materials

Raw materials

Preparation Products

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A-966492 Suppliers

AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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United States
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ApexBio Technology LLC
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+1-832-696-8203
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+1-832-641-3177
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info@apexbt.com
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United States
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Target molecule Corp.
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857-239-0968
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857-239-8801
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service1@targetmol.com
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Musechem
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+1-800-259-7612
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TargetMol Chemicals Inc.
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+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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United States
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InvivoChem
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+1-708-310-1919 +1-13798911105
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sales@invivochem.cn
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United States
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Cckinase, Inc.
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Aladdin Scientific
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TargetMol Chemicals Inc.
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ApexBio Technology
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BOC Sciences
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Alfa Chemistry
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Cayman Chemical Company
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Creative Enzymes
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934162-61-5, A-966492Related Search:


  • A966492;A 966492;A-966492
  • CS-903
  • A-966492
  • 2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide
  • A-966492(A 966492)
  • 2-{2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl}-1H-1,3-benzodiazole-7-carboxaMide
  • 2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide A-966492
  • A-966492, >=98%
  • 1H-Benzimidazole-7-carboxamide, 2-[2-fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-
  • A-966492 USP/EP/BP
  • A-966492 PARP inhibitor A966492
  • 2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide
  • (S)-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzo[d]imidazole-7-carboxamide
  • 934162-61-5
  • 931462-61-5
  • Inhibitor
  • Inhibitors
  • APIs