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SCH-772984

Chemical Structure : SCH-772984

CAS No.: 942183-80-4

SCH-772984 (SCH 772984;SCH772984)

Catalog No.: PC-45868Not For Human Use, Lab Use Only.

A novel potent and selective inhibitor of ERK1/ERK2 with IC50 of 4 nM/1 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A novel potent and selective inhibitor of ERK1/ERK2 with IC50 of 4 nM/1 nM, respectively; is highly selective, with only seven kinases of 300 showing >50% inhibition at 1 uM; prevents MEK-mediated ERK phosphorylation, reduces pCRAF S289/S296/S301 phosphorylation; has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRAS and induces tumor regressions in xenograft models.

Colon Cancer

Phase 1 Clinical

Physicochemical Properties

M.Wt 587.6742
Formula C33H33N9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 51 mg/mL

Chemical Name/SMILES

3-Pyrrolidinecarboxamide, 1-[2-oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-, (3R)-

References

1. Morris EJ, et al. Cancer Discov. 2013 Jul;3(7):742-50.

2. Wong DJ, et al. Mol Cancer. 2014 Aug 20;13:194.

3. Chaikuad A, et al. Nat Chem Biol. 2014 Oct;10(10):853-60.

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