OPB-171775 free base · Synonyms: OPB 171775 · OPB171775

OPB-171775 is a novel anticancer agent and demonstrated its potent efficacy against GISTs.

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

Target Molecular Glues Phosphodiesterase (PDE)

Research area Cancer

Purity HPLC >98%, ee>98% Stock Inquire

Data Sheet SDS COA

OPB-171775 structure

CAS No.: 2131210-15-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 550.00	BP-00882-100mg	In stock	Get quote
250 mg	USD 1,080.00	BP-00882-250mg	In stock	Get quote
500 mg	USD 1,720.00	BP-00882-500mg	In stock	Get quote
1 g	USD 2,750.00	BP-00882-1g	In stock	Get quote

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Description

OPB-171775 is a novel anticancer agent and demonstrated its potent efficacy against GISTs. OPB-171775 acts as a molecular glue between PDE3A and SLFN12 and exerts anticancer activity through the RNase activity of SLFN12.

Biological activity

In Vitro OPB-171775 (0.01-100 nM) shows a delayed onset of cytotoxicity compared to Imatinib (HY-15463) and induces significant cell death in SLFN12-expressing GIST-T1 cells. In Vivo OPB-171775 (0.1 mg/kg; p.o.; once daily; 21 days) reduces tumor volume and shows significant efficacy regardless of KIT mutation status in female NOD.CB17-Prkdcscid/J mice bearing patient-derived xenograft (PDX) models of gastrointestinal stromal tumors (GIST). OPB-171775 (0.03 mg/kg; p.o.; once daily; 21 days) combined Imatinib can lead to complete tumor regression in all mice bearing GS11353 PDX tumors.

Identifiers

SMILES: FC1=C(C=CC(OCC(C)(C)O)=C1F)C=2[C@H](C)CC(=O)NN2
InChIKey: GGUTYKLJESECBW-MRVPVSSYSA-N

Specifications

MW (average): 312.3118
Formula: C₁₅H₁₈F₂N₂O₃
CAS No.: 2131210-15-4
Physical state: Solid
Color: White to off-white
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 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Takaki, Emiri O et al. “A PDE3A-SLFN12 Molecular Glue Exhibits Significant Antitumor Activity in TKI-Resistant Gastrointestinal Stromal Tumors.” Clinical cancer research : an official journal of the American Association for Cancer Research vol. 30,16 (2024): 3603-3621. doi:10.1158/1078-0432.CCR-24-0096

Same target

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Same research area

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