PHA-767491 (hydrochloride)
PHA-767491 (hydrochloride)
CAS: 942425-68-5
Molecular Formula: C12H12ClN3O
PHA-767491 (hydrochloride) - Names and Identifiers
| Name | PHA-767491 (hydrochloride) |
| Synonyms | CAY-10572 HYDROCHLORIDE PHA-767491 (hydrochloride) |
| CAS | 942425-68-5 |
PHA-767491 (hydrochloride) - Physico-chemical Properties
| Molecular Formula | C12H12ClN3O |
| Molar Mass | 249.7 |
| Solubility | DMSO: < 9 mg/mL |
| Storage Condition | Inert atmosphere,Room Temperature |
| In vitro study | PHA-767491 20-fold selectivity for Cdk1, Cdk2 and GSK3-β,50-fold selectivity for MK2 and Cdk 5, and 100-fold selectivity for PLK1 and chk2. PHA-767491 inhibit the proliferation of a variety of human cell lines, IC50 ranges from 0.86 μm for SF-268 cells to 5.87 μm for K562 cells, and almost all cells are significantly induced to apoptosis in a p53-independent manner, whereas 5-FU or Gemcitabine acts on only a small subset of cell lines. Unlike current DNA synthesis inhibitors, 5 μm PHA-767491 blocks the initiation of DNA replication rather than the progression of replication forks due to specific inhibition of Cdc7 kinase and Mcm2 phosphorylation at cdc7-dependent Ser40 site. 3 M PHA-767491 treatment of ABT-737-resistant OCI-LY1 and SU-DHL-4 cells significantly reduced the level of up-regulated Mcl-1, probably because Cdk9 was inhibited, resulting in the recovery of sensitivity to ABT-737. A direct mitochondria-dependent pro-apoptotic effect was observed with 1 μm PHA-767491 on quiescent chronic lymphocytic leukemia (CLL) cells with an EC50 of 0.34-0.97 μm. 5 μm PHA-767491 treatment of CD154 and IL-4 stimulated proliferating CLL cells abrogated DNA synthesis by inhibiting Cdc7 rather than triggering cell death. |
| In vivo study | PHA-767491 treatment twice a day for 5 days significantly inhibited the growth of HL60 xenografts in a dose-dependent manner, with 20 mg/kg and 30 mg/kg treatment, TGI was 50% and 92%, respectively, and this effect was also significant in A2780, Mx-1, and HCT-116 xenograft models and DMBA-induced breast cancer, associated with Cdc7 inhibition, the phosphorylation of Mcm2 at the cdc7-dependent Ser40 site was subsequently reduced. |
PHA-767491 (hydrochloride) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.005 ml | 20.024 ml | 40.049 ml |
| 5 mM | 0.801 ml | 4.005 ml | 8.01 ml |
| 10 mM | 0.4 ml | 2.002 ml | 4.005 ml |
| 5 mM | 0.08 ml | 0.4 ml | 0.801 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Featured ProductsSpot supply
Product Name: CAY10572 Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: CAY-10572 hydrochloride Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PHA-767491 (hydrochloride) Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Product Name: PHA-767491 (hydrochloride) Visit Supplier Webpage Request for quotation
CAS: 942425-68-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 942425-68-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Featured ProductsSpot supply
Product Name: CAY10572 Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: CAY-10572 hydrochloride Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PHA-767491 (hydrochloride) Visit Supplier Webpage Request for quotationCAS: 942425-68-5
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Product Name: PHA-767491 (hydrochloride) Visit Supplier Webpage Request for quotation
CAS: 942425-68-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 942425-68-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History