A covalent inhibitor of K-RASG12C
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ARS1620

Item No. 27915

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]-2-propen-1-one
CAS Number
1698055-85-4
Molecular Formula
C21H17ClF2N4O2
Formula Weight
430.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
FC1=CC=CC(O)=C1C2=C(Cl)C=C(C(N3CCN(C(C=C)=O)CC3)=NC=N4)C4=C2F
InChi Code
InChI=1S/C21H17ClF2N4O2/c1-2-16(30)27-6-8-28(9-7-27)21-12-10-13(22)17(19(24)20(12)25-11-26-21)18-14(23)4-3-5-15(18)29/h2-5,10-11,29H,1,6-9H2
InChi Key
ZRPZPNYZFSJUPA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $130

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    5 mg

    $387

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    Cayman Chemical
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    Product Description

    ARS1620 is a covalent inhibitor of K-RASG12C (IC50 = <3 μM).1 It selectively inhibits growth of H358, MIA-PaCa2, and LU65 cancer cells that express K-RASG12C (IC50s = 150 nM) over H441, A549, and HCT116 cells expressing wild-type K-RAS (IC50s = >10 μM). ARS1620 (200 mg/kg) induces tumor regression in a MIA-PaCa2, but not an H441, mouse xenograft model. It also decreases tumor volume in patient-derived xenograft (PDX) mouse models expressing K-RASG12C, but not K-RASG12D or wild-type K-RAS.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Janes, M.R., Zhang, J., Li, L.-S., et al. Targeting KRAS mutant cancer cells with a covalent G12C-specific inhibitor. Cell 172(3), 578-589 (2018).