A covalent inhibitor of K-RasG12C
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AMG 510

Item No. 29465

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-pyrido[2,3-d]pyrimidin-2(1H)-one
CAS Number
2296729-00-3
Synonyms
  • Sotorasib
Molecular Formula
C30H30F2N6O3
Formula Weight
560.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
214 nm
SMILES
O=C1N=C(N2CCN(C(C=C)=O)CC2C)C3=CC(F)=C(C4=C(O)C=CC=C4F)N=C3N1C5=C(C(C)C)N=CC=C5C
InChi Code
InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3
InChi Key
NXQKSXLFSAEQCZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $29

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    5 mg

    $65

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    10 mg

    $101

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    25 mg

    $180

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    Cayman Chemical
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    Product Description

    AMG 510 is a covalent inhibitor of K-RasG12C.1 It inhibits EGF-induced phosphorylation of ERK1/2 in MIA PaCa-2 cells (IC50 = 68 nM). AMG 510 reduces the viability of MIA PaCa-2 cells that express K-RasG12C but not K-RasG12S-expressing A549 cells (IC50s = 5 and 36,500 nM, respectively). In vivo, AMG 510 (10, 30, and 100 mg/kg) reduces intratumor ERK1/2 phosphorylation and tumor volume in a MIA PaCa-2 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lanman, B.A., Allen, J.R., Allen, J.G., et al. Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors. J. Med. Chem. 63(1), 52-65 (2020).