10mM in DMSO für empfindliche chromatographische und analytische Workflows, die minimale Basislinieninterferenzen erfordern.
Store at -80°C Versand Dry ice packs + Cold packs. Genaue Spezifikationen finden Sie im chargenspezifischen COA.
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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
PHA-767491 (CAY10572, NMS 1116354) is a potent ATP-competitive dualCdc7/CDK9inhibitor withIC50of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fo
In vitro
PHA-767491 displays approximately 20-fold selectivity for Cdk1, Cdk2 and GSK3-β, 50-fold selectivity for MK2 and Cdk5 and 100-fold selectivity for PLK1 and CHK2. PHA-767491 inhibits cell proliferation in a variety of human cell lines with IC50 of 0.86 μM for SF-268 to 5.87 μM for K562, and significantly induces apoptosis in a p53-independent manner in almost all cell lines in contrast with 5-FU or gemcitabine which only works in a few of cell lines. Unlike current DNA synthesis inhibitors, PHA-767491 treatment at 5 μM blocks the initiation of DNA replication but not replication fork progression, due to specific inhibition of Cdc7 kinase and Mcm2 phosphorylation at the Cdc7-dependent Ser40 site. The up-regulated Mcl-1 levels in ABT-737-resistant OCI-LY1 and SU-DHL-4 cells can be significantly decreased by PHA-767491 treatment at 3 μM possibly due to the inhibition of Cdk9, leading to the restoration of the sensitivity to ABT-737. The direct mitochondrial dependent pro-apoptosis effect of PHA-767491 is also observed when applied at 1 μM in quiescent chronic lymphocytic leukemia (CLL) cells through the similar mechanism with EC50 of 0.34-0.97 μM. While in proliferating CLL cells stimulated by CD154 and interleukin-4, PHA-767491 treatment at 5 μM abolishes DNA synthesis by inhibiting Cdc7 rather than triggering cell death.
In vivo
Administration of PHA-767491 twice a day for 5 days significantly inhibits the growth of HL60 xenograft in a dose-dependent manner with TGI of 50% and 92% at dose of 20 mg/kg and 30 mg/kg, respectively, the effect of which is also marked in A2780, Mx-1, and HCT-116 xenograft models as well as the DMBA-induced mammary carcinomas, and correlates with Cdc7 inhibition and subsequently decreased phosphorylation of Mcm2 at the Cdc7-dependent site Ser40
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~ 20 μM
Incubation Time：24 or 72 hours
Powder Purity:≥99%
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| Lot Number | Certificate Type | Datum | Artikel |
|---|---|---|---|
 H2423240 | Certificate of Analysis | Jul 02, 2026 | P409268 |
| Löslichkeit | Solubility (25°C) In vitro DMSO: 63 mg/mL (199.79 mM); Ethanol: 1 mg/mL (3.17 mM); Water: Insoluble; |
|---|
