Basroparib free base · Synonyms: STP1002

Basroparib is a potent poly polymerase inhibitor.

For research use only. Not for human or veterinary use.

Target PARP

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Basroparib structure

CAS No.: 1858179-75-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 560.00	BP-02158-10mg	In stock	Get quote
25 mg	USD 1,100.00	BP-02158-25mg	In stock	Get quote
50 mg	USD 1,720.00	BP-02158-50mg	In stock	Get quote
100 mg	USD 2,800.00	BP-02158-100mg	In stock	Get quote

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Description

Basroparib is a potent poly (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity.

Biological activity

In Vitro Basroparib (1.25-20 μM; 72 h) has synergistic inhibitory potency (CI <1) with the MEK inhibitor Trametinib (HY-10999) (3.125-50 nM; 72 h) in cell viability experiments of KRAS-G12V/D mutant colorectal cancer cell lines (such as SW480, SW620). Basroparib (5 μM; 14 d) significantly inhibits the colony formation of KRAS-G12V mutant cells (SW480, SW620), with enhanced inhibitory effect combined with Trametinib (5 nM; 14 d). Basroparib (5 μM; 7 d) inhibits the growth of 3D clonal spheroids of KRAS-G12V mutant cells, and significantly reduced the spheroid diameter combined with Trametinib (0.1 nM; 7 d). Basroparib (5 μM; 48 h) upregulates the AXIN1/2 protein level and downregulates the expression of phosphorylated β-catenin and p-ERK in KRAS-G12V mutant cells (SW480). Basroparib (5 μM; 48 h) reduces the nuclear active β-catenin aggregation in KRAS-G12V mutant cells. In Vivo Basroparib (10 mg/kg; oral; once daily; for 27-28 days) combined with trametinib (0.5 mg/kg; oral; once daily), significantly inhibits tumor growth and downregulates β-catenin and p-ERK expression in the KRAS-G12V mutant SW480/SW620 colorectal cancer model in female nude mice. Basroparib (10 mg/kg; oral; once daily; for 4 weeks) combined with trametinib (0.5 mg/kg; oral; once daily), delays tumor regrowth in the trametinib-resistant SW620 tumor model in female nude mice and prolongs the survival of mice.

Identifiers

SMILES: O=C1N=C(N2CCN(CC2)C3=C(C=C(C=C3F)OCCOC)F)NC4=C1N=NN4C
InChIKey: ALDDPEMJJONRDI-UHFFFAOYSA-N

Specifications

MW (average): 421.4012
Formula: C₁₈H₂₁F₂N₇O₃
CAS No.: 1858179-75-5
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[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.

[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.

Same target

Search PARP

Same research area

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