1858179-75-5
Chemical Structure
Basroparib
Synonym(s): STP1002
- CAS No.: 1858179-75-5
- Formula:C18H21F2N7O3
- Molecular Weight:421.40
IUPAC Name: 5-(4-(2,6-difluoro-4-(2-methoxyethoxy)phenyl)piperazin-1-yl)-3-methyl-3,4-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
InChIKey: ALDDPEMJJONRDI-UHFFFAOYSA-N
SMILES: O=C1N=C(N2CCN(CC2)C3=C(C=C(C=C3F)OCCOC)F)NC4=C1N=NN4C
Biological Activity: Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Basroparib | 98.91% | Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Kwon YJ, et al. Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer. Biochem Pharmacol. 2025 May;235:116842. [Content Brief]
- [2]. Kim, Uk-Il, et al. Formulation development of basroparib as a first-in-class tankyrase inhibitor using a microprecipitated bulk powder approach. Journal of Pharmaceutical Investigation (2025): 1-11.
- [3]. Bai YR, et al. The recent advance and prospect of poly(ADP-ribose) polymerase inhibitors for the treatment of cancer. Med Res Rev. 2024 Aug 24. [Content Brief]
Keywords
