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Cat. No. Product Name CAS No. Information
PC-43380

Cobimetinib R-enantiomer

934660-94-3

Cobimetinib R-enantiomer (GDC-0973; XL518) is the R-enantiomer of Cobimetinib (GDC-0973; XL518), which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).

PC-43369

Cobimetinib

934660-93-2

Cobimetinib (GDC-0973, XL-518) is a potent, selective MEK inhibitor with IC50 of 4.2 nM for MEK1; shows excellent selectivity against mTOR, DNA-dependent protein kinase (DNA-PK), and a panel of more than 228 kinases; shows strong cellular potency in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines, triggers robust apoptosis and tumor growth inhibition in vivo combined with PI3K inhibitor GDC-0941.

Skin Cancer

Approved

PC-62664

Vacquinol-1

5428-80-8

Vacquinol-1 (NSC 13316) is a MKK4 (MAP2K4, MEK4) activator that induces vacuolization, induces ATP depletion in glioblastoma cells (IC50 = 3.14 uM) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells; induces rapid and specific cell death of glioma cells via membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture; shows good brain penetrance and excellent pharmacokinetics; orally bioactive.

PC-43541

TAK-733

1035555-63-5 TAK-733 (TAK733,TAK 733) is a potent, selective, allosteric inhibitor of MEK with IC50 of 3.2 nM (MEK1); shows selectivity for MEK1 over a panel of 18 kinases, receptors, and ion channels at uM; inhibits ERK phosphorylation in vitro with EC50 of 1.9 nM, also inhibits proliferation of A375 and COLO 205 cells with IC50 of 3.1 nM and 2.1 nM, respectively; as well as 14 cutaneous melanoma cell lines (IC50s=<1-10 nM), espectially in those with B-RAFV600E mutations; demonstrates antitumor activity in multiple mouse xenograft models.

Solid Tumors

Phase 1 Discontinued

PC-43379

Cobimetinib racemate

934662-91-6 Cobimetinib racemate is the racemate form of Cobimetinib (GDC-0973, XL518), which is a potent, highly selective inhibitor of MEK1/2.
PC-43047

OTS-964

1338545-07-5 OTS-964 is a dimethylated derivative of OTS514 and potent, selective TOPK inhibitor with IC50 of 28 nM, exhibits excellent in vivo efficacy with liposomal formulation; inhibits the growth of TOPK-positive cells with low IC50 values (A549 IC50=31 nM), decreases autophosphorylation of TOPK (Thr9), as well as phosphorylation of histone H3 (Ser10), in both T47D and LU-99 cells; the liposomal OTS964 causes complete regression of tumors without any detectable toxicity in the xenograft models.
PC-42877

PD318088

391210-00-7 PD318088 is a potent, non-ATP competitive, allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

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