Drug Information

Drug (ID: DG01632) and It's Reported Resistant Information

• Name: EBI-907
• Synonyms: CHEMBL3751896; EBI-907; 1581764-31-9; SCHEMBL15577685; BDBM50140046; SB19682
• Target: .; NOUNIPROTAC; [1]
• Formula: 8
• IsoSMILES: COC1=C(C=C2C=NC3=NNC(=C3C2=C1)C4CC4)C5=C(C=CC(=C5Cl)NS(=O)(=O)CCCF)F
• InChI: InChI=1S/C23H21ClF2N4O3S/c1-33-18-10-14-13(11-27-23-20(14)22(28-29-23)12-3-4-12)9-15(18)19-16(26)5-6-17(21(19)24)30-34(31,32)8-2-7-25/h5-6,9-12,30H,2-4,7-8H2,1H3,(H,27,28,29)
• InChIKey: JSKJFDXTKYWPAH-UHFFFAOYSA-N
• PubChem CID: 73427153

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Melanoma [ICD-11: 2C30]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]

• Molecule Alteration: Missense mutation; p.V600E (c.1799T>A)
• Sensitive Disease: Melanoma [ICD-11: 2C30.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A375 cells; Skin; Homo sapiens (Human); CVCL_0132
• In Vitro Model: SW-480 cells; Colon; Homo sapiens (Human); CVCL_0546
• In Vitro Model: Colo-205 cells; Ascites; Homo sapiens (Human); CVCL_0218
• In Vitro Model: Calu-6 cells; Lung; Homo sapiens (Human); CVCL_0236
• In Vivo Model: Nu/Nu Colo-205 xenograft mouse model; Nu/Nu A357 xenograft mouse model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CellTiter-Glo luminescent cell viability assay

References

• Ref 1: EBI-907, a novel BRAF(V600E) inhibitor, has potent oral anti-tumor activity and a broad kinase selectivity profileCancer Biol Ther. 2016;17(2):199-207. doi: 10.1080/15384047.2016.1139231. Epub 2016 Jan 25.