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Home > Chemicals > Amino Acids and Derivatives > M2698 (MSC2363318A)

M2698 (MSC2363318A)

MSC2363318A, M-2698

Catalog No. Product Name Size List Price (US$) Quantity
APIM050046 M2698 (MSC2363318A) 5 mg 120.00
APIM050046 M2698 (MSC2363318A) 10 mg 175.00
APIM050046 M2698 (MSC2363318A) 50 mg 485.00
APIM050046 M2698 (MSC2363318A) 100 mg 795.00
Description

Background Information:

M2698 (MSC2363318A) is an orally bioavailable, BBB penetrable p70S6K/Akt dual inhibitor, and is highly potent in vitro (IC50 1 nM for p70S6K, Akt1 and Akt3 inhibition; IC50 17 nM for pGSK3β indirect inhibition) and in vivo (IC50 15 nM for pS6 indirect inhibition), and relatively selective (only 6/264 kinases had an IC50 within 10-fold of p70S6K). Orally administered M2698 crossed the blood-brain barrier in rats and mice, with brain tumor exposure 4-fold higher than non-disease brain. Dose-dependent inhibition of target substrate phosphorylation was observed in vitro and in vivo, indicating that M2698 blocked p70S6K to provide potent PAM pathway inhibition while simultaneously targeting Akt to overcome the compensatory feedback loop. M2698 demonstrated dose-dependent tumor growth inhibition in mouse xenograft models derived from PAM pathway-dysregulated human triple-negative (MDA-MB-468) and Her2-expressing breast cancer cell lines (MDA-MB-453 and JIMT-1), and reduced brain tumor burden and prolonged survival in mice with orthotopically implanted U251 glioblastoma (ref 1).

Reference:

1. A Machl, et al, M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier, Am J Cancer Res. 2016 Mar 15;6(4):806-18. eCollection 2016.

APIM050046: M2698 (MSC2363318A)

CAS No.: 1379545-95-5.
Molecular Formula: C21H19ClF3N5O.
Molecular Weight: 449.9 (or, refer to Certificate of Analysis, batch-specific).
Purity: 99.8-100% by achiral and chiral HPLCs.
QC: HPLC-MS, 1H-NMR, Chiral HPLC and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.

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