BAL3833(TBAP-001)

  Cat. No.:  DC40000   Featured
Chemical Structure
1777832-90-2
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Field of application
BAL3833 (also known as CCT3833) is an orally available small-molecule panRAF/SRC kinase inhibitor targeting cell proliferation signaling pathways that are associated with tumor growth and resistance development to current therapies. Data from preclinical studies suggest that this class of compounds, targeting the BRAF, CRAF and SRC family kinases, is active in diverse patient-derived melanoma models with intrinsic or acquired resistance to currently marketed BRAF-specific as well as MEK inhibitor therapies.8 Moreover, activity of BAL3833 has also been demonstrated in KRAS-driven cancer models, including non-small cell lung cancer, colorectal cancer and pancreatic cancer.9 BAL3833 has been progressed into a phase 1 study in adult patients with advanced solid tumors including metastatic melanoma.
Cas No.: 1777832-90-2
Chemical Name: Urea, N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-fluorophenyl]-N'-[3-(1,1-dimethylethyl)-1-(3-fluorophenyl)-1H-pyrazol-5-yl]-
Synonyms: BAL3833;BAL-3833;BAL 3833;CCT3833;CCT-3833;CCT 3833
SMILES: O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=CC(F)=C2)NC3=CC=C(OC4=C(N=C5)C(NC5=O)=NC=C4)C=C3F
Formula: C27H23F2N7O3
M.Wt: 531.51
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: G. Saturno et al. Therapeutic efficacy of the paradox-breaking panRAF and SRC drug CCT3833/BAL3833 in KRAS-driven cancer models. American Association for Cancer Research (AACR) annual meeting 2016, abstract LB-212
Description: BAL3833(TBAP-001), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay[1].
Target: IC50: 62 nM (BRAF V600E kinase assay), 18 nM (Cell-Based Phosho-ERK Assay)[1].
In Vitro: BAP-001 (Synthesis 13) exhibits IC50 values of 178 nM (A375), 62 nM (WM266.4), 72 nM (UACC62), 93 nM (LOX INVI), 590 nM (HT 29), 43 nM (COLO225), 690 nM (RKO), 490 nM (Mawi), 390 nM (WiDr), 480 nM (Colo741), 480 nM (SW620), 600 nM (HCT116), 390 nM (SKMEL2), 710 nM (D04), 390 nM (WM1361), 1150 nM (PDAC R172H (p53 mut)), 290 nM (MiaPaCa) and 490nM (RPMI8226) in different cancer cell lines[1].
References: [1]. Caroline Joy, et al. 1 -(5-TERT-BUTYL-2-ARYL-PYRAZOL-3-YL)-3-[2-FLUORO-4-[(3-OXO-4H-PYRIDO[2,
MSDS
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MSDS_20419_DC40000_1777832-90-2
COA
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