Dapolsertib

Chemical Information
Dapolsertib is an orally available inhibitor of PIM family serine/threonine protein kinases and mutant forms of FMS-related tyrosine kinase 3 (FLT3; STK1) with potential antineoplastic activity. Upon oral administration, dapolsertib binds to and inhibits the kinase activities of PIM-1, -2 and -3, and mutant forms of FLT3, which may result in the interruption of the G1/S phase cell cycle transition, an inhibition of cell proliferation, and an induction of apoptosis in tumor cells that overexpress PIMs or express mutant forms of FLT3. FLT3, a tyrosine kinase receptor that is overexpressed or mutated in various cancers, plays a role in signaling pathways that regulate hematopoietic progenitor cell proliferation, and in leukemic cell proliferation and survival. PIM kinases, downstream effectors of many cytokine and growth factor signaling pathways, including the FLT3 signaling pathway, play key roles in cell cycle progression and apoptosis inhibition and may be overexpressed in various malignancies.
| CAS Number | 1616359-00-2 |
| PubChem CID | 76286825 |
| IUPAC Name | 5,6-dibromo-4-nitro-2-piperidin-4-yl-1-propan-2-ylbenzimidazole |
| Molecular Formula | C15H18Br2N4O2 |
| Molecular Weight | 446.14 |
| XLogP | 3.5 |
| Topological Polar Surface Area | 75.7 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 2 |
| Heavy Atom Count | 23 |
| Formal Charge | 0 |
| Complexity | 442 |
| Property | Value |
|---|---|
| Molecular Weight | 446.14 |
| XLogP3 | 3.5 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 2 |
| Exact Mass | 445.97760 |
| Monoisotopic Mass | 443.97965 |
| Topological Polar Surface Area | 75.7 Ų |
| Heavy Atom Count | 23 |
| Formal Charge | 0 |
| Complexity | 442 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
Alternative Products
| Catalog | Name |
|---|---|
| T39085-01 | Dapolsertib |
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