A PARP1 and PARP2 inhibitor
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A-966492

Item No. 26378

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[2-fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide
CAS Number
934162-61-5
Molecular Formula
C18H17FN4O
Formula Weight
324.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
NC(C1=C(NC(C2=CC=C([C@H]3NCCC3)C=C2F)=N4)C4=CC=C1)=O
InChi Code
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
InChi Key
AHIVQGOUBLVTCB-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $288

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    25 mg

    $587

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    Cayman Chemical
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    Product Description

    A-966492 is a dual inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (Kis = 1 and 1.5 nM, respectively).1 It reduces tumor growth by 46 and 92% in an MX-1 mouse xenograft model when administered at doses of 100 and 200 mg/kg per day, respectively.1 A-966492 also reduces tumor growth in a B16/F10 murine melanoma model when administered in combination with temozolomide (Item No. 14163).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Penning, T.D., Zhu, G.D., Gong, J., et al. 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. 53(8), 3142-3153 (2010).