SCH772984
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MedKoo CAT#: 406578

CAS#: 942183-80-4

Description: SCH772984 is an potent and selective ERK inhibitor with potential anticancer activity. SCH722984 showed activity against BRAF mutant, NRAS mutant and wild-type melanoma. Combining vemurafenib and SCH722984 in BRAF mutant melanoma was synergistic in a majority of cell lines and significantly delayed the onset of acquired resistance in long term in vitro assays. Therefore, SCH772984 may be clinically applicable as a treatment for non-BRAF mutant melanoma or in BRAF-mutant melanoma with innate or acquired resistance, alone or in combination with BRAF inhibitors.


Chemical Structure

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SCH772984
CAS# 942183-80-4

Theoretical Analysis

MedKoo Cat#: 406578
Name: SCH772984
CAS#: 942183-80-4
Chemical Formula: C33H33N9O2
Exact Mass: 587.27572
Molecular Weight: 587.67422
Elemental Analysis: C, 67.44; H, 5.66; N, 21.45; O, 5.44

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Same day
25.0mg USD 290.0 Same day
50.0mg USD 550.0 Same day
100.0mg USD 950.0 Same day
200.0mg USD 1550.0 Same day
500.0mg USD 2750.0 Same day
1.0g USD 3950.0 Same day
2.0g USD 5450.0 Same day
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Synonym: SCH772984; SCH-772984; SCH 772984.

IUPAC/Chemical Name: (R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide

InChi Key: HDAJDNHIBCDLQF-RUZDIDTESA-N

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

SMILES Code: O=C([C@H]1CN(CC(N2CCN(C3=CC=C(C4=NC=CC=N4)C=C3)CC2)=O)CC1)NC5=CC6=C(NN=C6C7=CC=NC=C7)C=C5

Appearance: Yellow Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO (10mg/mL).

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 587.67422 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Chaikuad A, M C Tacconi E, Zimmer J, Liang Y, Gray NS, Tarsounas M, Knapp S. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol. 2014 Oct;10(10):853-60. doi: 10.1038/nchembio.1629. Epub 2014 Sep 7. PubMed PMID: 25195011.

2: Wong DJ, Robert L, Atefi MS, Lassen A, Avarappatt G, Cerniglia M, Avramis E, Tsoi J, Foulad D, Graeber TG, Comin-Anduix B, Samatar A, Lo RS, Ribas A. Antitumor activity of the ERK inhibitor SCH722984 against BRAF mutant, NRAS mutant and wild-type melanoma. Mol Cancer. 2014 Aug 20;13:194. doi: 10.1186/1476-4598-13-194. PubMed PMID: 25142146; PubMed Central PMCID: PMC4155088.

3: Nissan MH, Rosen N, Solit DB. ERK pathway inhibitors: how low should we go? Cancer Discov. 2013 Jul;3(7):719-21. doi: 10.1158/2159-8290.CD-13-0245. PubMed PMID: 23847348.

4: Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24. PubMed PMID: 23614898.



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