FHD-909
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3008577-34-9
- Formel: C29H25F2N5O5S
- Molecular Weight:593.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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SMARCA2 0.0025 μM (IC50) |
SMARCA4 |
FHD-909 (LY4050784) (10 days) potently and selectively inhibits proliferation of SMARCA4-mutant non-small cell lung cancer cell lines in vitro, with the median IC50 for SMARCA4-mutant lines being 33-fold lower than that for SMARCA4-wildtype lines[1].
FHD-909 (0.1-100 nM) exhibits additive and synergistic anti-proliferative activity when combined with Cisplatin (HY-17394), Paclitaxel (HY-B0015) or Pemetrexed (HY-10820) in A549 SMARCA4-mutant non-small cell lung cancer cell lines in vitro[1].
FHD-909 (0.1-100 nM with olomorasib; 0.1-100 nM with LY4066434) exhibits synergistic anti-proliferative activity when combined with Olomorasib (HY-132980) or LY4066434 in NCI-H2030 SMARCA4-mutant, KRASG12C non-small cell lung cancer cell lines in vitro[1].
FHD-909 (0.1-1000 nM in PATU-8988T cells; 0.1-1000 nM in SNU-407 cells) exhibits synergistic anti-proliferative activity when combined with LY3962673 in PATU-8988T pancreatic ductal adenocarcinoma cell lines and SNU-407 colorectal cancer cell lines in vitro[1].
FHD-909 (1-10000 nM in A549 cells; 1-10000 nM in PATU-8988T cells) exhibits synergistic anti-proliferative activity when combined with LY4066434 in A549 non-small cell lung cancer cell lines and PATU-8988T pancreatic ductal adenocarcinoma cell lines in vitro[1].
FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and is 35.69-fold selective for BRM over purified BRG1 ATPase[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
FHD-909 (60 mg/kg; p.o.; BID; 28 days) enhances the antitumor activity of Cisplatin and Pemetrexed combination chemotherapy, leading to tumor regression in SMARCA4G12C-mutant NSCLC xenografts[1].
FHD-909 (40 mg/kg; p.o.; BID; 28 days) enhances the antitumor activity of Cisplatin and Paclitaxel combination chemotherapy, leading to tumor regression in SMARCA4G12C-mutant NSCLC xenografts[1].
FHD-909 (20, 40 mg/kg; p.o.; BID; study day 22 to 49) sensitizes SMARCA4G12C-mutant NSCLC xenografts to Pembrolizumab (HY-P9902), resulting in enhanced antitumor activity compared to monotherapy[1].
FHD-909 (40 mg/kg; p.o.; BID; 28 days) combined with Olomorasib produces synergistic antitumor activity and sustained tumor regression in SMARCA4/KRASG12C co-mutant NSCLC xenografts[1].
FHD-909 (40 mg/kg; p.o.; BID; 28 days) combined with LY4066434 produces synergistic antitumor activity and sustained tumor regression in SMARCA4/KRASG12S co-mutant NSCLC xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3008577-34-9
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Molecular Weight 593.60
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Formel C29H25F2N5O5S
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SMILES
O=C(C1=CC(F)=C(OCC[C@@H](S2(=O)=O)F)C2=C1)NCC3=CC4=C(C=N3)C=CC(N5C6=NC(C7CC7)=CC=C6OCC5)=N4
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Synonyms
LY4050784
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)