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PRT3789

PRT3789 is a SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4) . PRT3789 shows synergistic anti-proliferation effects with Adagrasib (HY-130149) in cancer cells. PRT3789 inhibits SMARCA4-mutated lung cancer proliferation. PRT3789 inhibits tumor growth in SMARCA4-deleted NSCLC models. Pink: SMARCA4 ligand (HY-44824) ; Blue: VHL ligand (HY-159465) ; Black: linker; VHL ligand+linker (HY-172738) [1].

Product Specifications

CAS Number

[2755761-78-3]

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/smarca2-degrader-17.html

Smiles

CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)C4=CC(O[C@@H](C)CN5CC[C@H](C5)N6CCN7C8=C(NC[C@H]7C6)N=NC(C9=C(C=CC=C9)O)=C8)=NO4)=O)O)=O)C

Molecular Formula

C47H58N10O6S

Molecular Weight

891.09

References & Citations

[1]Koichi Ito, et al. Improved treatment of cancers using combinations of smarca2 degraders and kras targeting therapies. Patent. WO2024076985A2

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 2

Available Sizes

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