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);A-966492, 10 mM in DMSO;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
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
InChI: InChI=1S/C18H17FN4O/c19-13-9-10(14-5-2-8-21-14)6-7-11(13)18-22-15-4-1-3-12(17(20)24)16(15)23-18/h1,3-4,6-7,9,14,21H,2,5,8H2,(H2,20,24)(H,22,23)/t14-/m0/s1
InChIKey: AHIVQGOUBLVTCB-AWEZNQCLSA-N
SMILES: C1(C2=CC=C([C@@H]3CCCN3)C=C2F)NC2=C(C(N)=O)C=CC=C2N=1

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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

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.

in vivo

A-966492 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In addition, A-966492 has excellent pharmaceutical properties and has demonstrated in vivo efficacy in preclinical mouse tumor models in combination with TMZ and carboplatin, as well as single agent activity in a BRCA1-deficient MX-1 tumor model. A-966492 is further characterized in Sprague Dawley rats, beagle dogs, and cynomolgus monkeys, with A-966492 demonstrating oral bioavailabilities of 34 72% and half-lives of 1.7 1.9 hours. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy^[1].

IC 50

PARP-1: 1 nM (Ki); PARP-2: 1.5 nM (Ki)

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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934162-61-5, A-966492Related Search:

PF-01367338 Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro- Saracatinib Veliparib 4-iodo-3-nitrobenzamide Olaparib

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

A-966492, 10 mM in DMSO

(s)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1h-benzo[d]imidazole-4-carboxamide

934162-61-5

931462-61-5

Inhibitor

Inhibitors

APIs