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SCH 772984

Item № 19166
CAS № 942183-80-4
Purity ≥95%
product image
                (CAS 942183-80-4)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $29.00 0.00
     5 mg $131.00 0.00
     10 mg $232.00 0.00

Pricing updated 2019-05-23. Prices are subject to change without notice.

Description

The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.1 SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).2 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.2 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.3

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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
A crystalline solid
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Seger, R., and Krebs, E.G. The MAPK signaling cascade The FASEB Journal 9, 726-735 (1995).

2. 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).

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

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