MedKoo Cat#: 128886 | Name: P11−2

Description:

WARNING: This product is for research use only, not for human or veterinary use.

P11−2 is a MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. P11−2 exhibited robust antitumor activity against MV4−11cells (IC50 = 45 nM) by efficiently degrading MNK1 (DC50 = 11.92nM, Dmax > 96%) mediated by the ubiquitin-proteasome system. Notably, P11−2 does not degrade MNK2, which played an important role in maintaining normal function. Moreover, P11−2significantly suppressed the phosphorylation of eIF4E (IC50 =22.07 nM), induced apoptosis, and arrested the cell cycle at the G1phase. In addition, P11−2 exhibited favorable PK profiles and robust antitumor effects in the xenograft model.

Chemical Structure

P11−2
P11−2
CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128886

Name: P11−2

CAS#: N/A

Chemical Formula: C35H38N6O6S

Exact Mass: 670.2574

Molecular Weight: 670.79

Elemental Analysis: C, 62.67; H, 5.71; N, 12.53; O, 14.31; S, 4.78

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
P11−2; P112; P11 2
IUPAC/Chemical Name
1-(7-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-7-oxoheptanoyl)-N-(5-phenylthiazol-2-yl)piperidine-4-carboxamide
InChi Key
SSXJSBLKMHBTEA-UHFFFAOYSA-N
InChi Code
InChI=1S/C35H38N6O6S/c42-29(37-26-11-7-10-24-25(26)21-41(34(24)47)27-14-15-30(43)38-33(27)46)12-5-2-6-13-31(44)40-18-16-23(17-19-40)32(45)39-35-36-20-28(48-35)22-8-3-1-4-9-22/h1,3-4,7-11,20,23,27H,2,5-6,12-19,21H2,(H,37,42)(H,36,39,45)(H,38,43,46)
SMILES Code
O=C(C1CCN(C(CCCCCC(NC2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)=O)=O)CC1)NC5=NC=C(C6=CC=CC=C6)S5
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 670.79 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
Discovery of P11–2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer Zhongcheng Yang, Yuxia Liu, Zibin Liao, Lianru Chen, Zhiling Liang, Luyong Zhang, and Zheng Li Journal of Medicinal Chemistry Article ASAP DOI: 10.1021/acs.jmedchem.5c00062