STP1002 | TNKS1/2 inhibitor | Probechem Biochemicals

Chemical Structure : STP1002

STP1002 (Basroparib, STP 1002)

Catalog No.: PC-49120Not For Human Use, Lab Use Only.

STP1002 (Basroparib) is a potent, selective and orally active inhibitor of tankyrase 1/2 (TNKS1/2) with IC50 of 5.8/3.2 nM, respectively, shows excellent selectivity against PARP1/2 compared to XAV939.

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Biological Activity

STP1002 (Basroparib) is a potent, selective and orally active inhibitor of tankyrase 1/2 (TNKS1/2) with IC50 of 5.8/3.2 nM, respectively, shows excellent selectivity against PARP1/2 compared to XAV939.

STP1002 does not inhibit members of the poly (ADP-ribose) polymerase 1/2 (PARP1/2), does not substantially modulates receptor binding for 68 receptors, inhibits enzyme activity or have cellular agonist or antagonist function for 468 panels in a battery of radioligand binding assays at 2 uM and 468 human kinases at 1 uM.

STP1002 significantly inhibits Wnt/b-catenin signalling (IC50=8.3 nM) compared to XAV939 and IWR-1.

STP1002 exerts antitumour activity by stabilising AXINs and antagonising the Wnt/β-catenin pathway in a subset of APC-mutated CRC cell lines, but not in inhibitor-resistant cells and APC-wild-type CRC cell lines.

STP1002 stabilises AXINs in adenomatous polyposis coli-mutated colorectal cancer cell lines and in vivo.

STP1002 (10-30 mg/kg/QD, p.o.) inhibits tumour growth of APC-mutated CRC xenograft animal models but not of APC-wild type models in a dose-dependent manner, also inhibits tumour growth in APC-mutated CRC patient-derived tumour xenograft models.

STP1002 shows no significant on-target toxicity in the GI tract compared to G007-LK.

Physicochemical Properties

M.Wt	421.409
Formula	C18H21F2N7O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(4-(2,6-difluoro-4-(2-methoxyethoxy)phenyl)piperazin-1-yl)-3-methyl-3,6-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one

References

1. Dong Young Kim, et al. Eur J Cancer. 2022 Jul 15;173:41-51.

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STP1002 (Basroparib, STP 1002)

Biological Activity

Physicochemical Properties

References

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