A selective inhibitor of ERK1/2
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SCH 772984

Item No. 19166

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R)-1-[2-oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide
CAS Number
942183-80-4
Molecular Formula
C33H33N9O2
Formula Weight
587.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS (pH 7.2) (1:5): 0.1 mg/mlDMSO: 1 mg/ml
λmax
233, 323 nm
SMILES
O=C(CN1C[C@H](C(NC2=CC=C(NN=C3C4=CC=NC=C4)C3=C2)=O)CC1)N(CC5)CCN5C(C=C6)=CC=C6C7=NC=CC=N7
InChi Code
InChI=1S/C33H33N9O2/c43-30(42-18-16-41(17-19-42)27-5-2-24(3-6-27)32-35-11-1-12-36-32)22-40-15-10-25(21-40)33(44)37-26-4-7-29-28(20-26)31(39-38-29)23-8-13-34-14-9-23/h1-9,11-14,20,25H,10,15-19,21-22H2,(H,37,44)(H,38,39)/t25-/m1/s1
InChi Key
HDAJDNHIBCDLQF-RUZDIDTESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    Product Description

    SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).1 It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 µM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS.1 It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Morris, E.J., Jha, S., Restaino, C.R., et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 3(7), 742-750 (2013).

    2. Cahikaud, A., Tacconi, E., Zimmer, J., et al. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat. Chem. Biol. 10(10), 853-860 (2014).