WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205792
CAS#: 1184173-73-6 (free base)
Description: MK-8353, also known as SCH900353, is a potent and orally active ERK1/2 inhibitor and anticancer drug candidate currently being developed by Schering-Plough. MK-8353 exhibited comparable potency with SCH772984 across various preclinical cancer models.
MedKoo Cat#: 205792
CAS#: 1184173-73-6 (free base)
Chemical Formula: C37H41N9O3S
Exact Mass: 691.3053
Molecular Weight: 691.855
Elemental Analysis: C, 64.23; H, 5.97; N, 18.22; O, 6.94; S, 4.63
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Related CAS #: 1184173-73-6 (free base) 1951448-73-9 (HCl) 1951448-74-0 (HCl hydrate) 1951428-60-6 (hydrate) 1951428-61-7 (x HCl)
Synonym: SCH900353; SCH-900353; SCH 900353; MK-8353; MK 8353; MK8353.
IUPAC/Chemical Name: (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide
InChi Key: KPQQGHGDBBJGFA-QNGWXLTQSA-N
InChi Code: InChI=1S/C37H41N9O3S/c1-24(2)49-32-12-9-28(20-38-32)34-30-19-29(10-11-31(30)41-42-34)40-36(48)37(50-4)15-18-45(22-37)21-33(47)46-16-13-26(14-17-46)25-5-7-27(8-6-25)35-39-23-44(3)43-35/h5-13,19-20,23-24H,14-18,21-22H2,1-4H3,(H,40,48)(H,41,42)/t37-/m0/s1
SMILES Code: O=C(CN1CC[C@@](SC)(C(NC2=CC=C(NN=C3C4=CC=C(OC(C)C)N=C4)C3=C2)=O)C1)N5CCC(C6=CC=C(C7=NN(C)C=N7)C=C6)=CC5
Appearance: 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
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
The following data is based on the product molecular weight 691.855 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.
|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|
1: Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC,
Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS 3rd, Zhang D, Miselis NR, Samatar
AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P,
Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty
KT. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients
with advanced solid tumors. JCI Insight. 2018 Feb 22;3(4). pii: 92352. doi:
10.1172/jci.insight.92352. [Epub ahead of print] PubMed PMID: 29467321.
Constitutive activation of ERK1/2 occurs in various cancers, and its reactivation is a well-described resistance mechanism to MAPK inhibitors. ERK inhibitors may overcome the limitations of MAPK inhibitor blockade.