SML3399
CHZ868
≥98% (HPLC)
Synonym(s):
CHZ 868, CHZ-868, N-(4-((2-((2,4-Difluorophenyl)amino)-1,4-dimethyl-1H-benzo[d]imidazol-5-yl)oxy)pyridin-2-yl)acetamide, N-[4-[[2-[(2,4-Difluorophenyl)amino]-1,4-dimethyl-1H-benzimidazol-5-yl]oxy]-2-pyridinyl]acetamide, NVP-CHZ 868, NVP-CHZ-868, NVP-CHZ868
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About This Item
Empirical Formula (Hill Notation):
C22H19F2N5O2
CAS Number:
Molecular Weight:
423.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to pink
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Related Categories
Biochem/physiol Actions
Orally active, type II tyrosine kinase I inhibitor against VEGFR1/2 (FLT1/KDR), PDGFR1/2, KIT, and ROS1 oncogenic fusions/mutations-drivent growth.
CHZ868 is a type II tyrosine kinase inhibitor that exhibits potent antiproliferation activity against VEGFR1/2 (FLT1/KDR), PDGFR1/2, KIT, and ROS1 TEL fusions-, as well as JAK2 V617F, but not RAF V600E, mutation-driven oncogenic growth (IC50 = 2/11, 4/23, 16, 40, 51 against respective BaF3 transformants) via stablizing target kinases in the inactive “DFG-out” conformation. CHZ868 overcomes Type I JAK inhibitor resistance of JAK2/MPN mutant MPN and JAK2 I682F/CRLF2-rearranged B-ALL cells both in cultures and in mice in vivo (30-40 mg/kg/day p.o.). Comparing to BBT594, CHZ868 is ineffective against BCR-ABL, TEL-FLT3, TEL-RET.
CHZ868 is a type II tyrosine kinase inhibitor that exhibits potent antiproliferation activity against VEGFR1/2 (FLT1/KDR), PDGFR1/2, KIT, and ROS1 TEL fusions-, as well as JAK2 V617F, but not RAF V600E, mutation-driven oncogenic growth (IC50 = 2/11, 4/23, 16, 40, 51 against respective BaF3 transformants) via stablizing target kinases in the inactive “DFG-out” conformation. CHZ868 overcomes Type I JAK inhibitor resistance of JAK2/MPN mutant MPN and JAK2 I682F/CRLF2-rearranged B-ALL cells both in cultures and in mice in vivo (30-40 mg/kg/day p.o.). Comparing to BBT594, CHZ868 is ineffective against BCR-ABL, TEL-FLT3, TEL-RET.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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miR-204 inhibits angiogenesis and promotes sensitivity to cetuximab in head and neck squamous cell carcinoma cells by blocking JAK2-STAT3 signaling
Biomedicine and Pharmacotherapy, 99, 278-285 (2018)
How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study
Scientific Reports, 7(1), 9088-9088 (2017)
CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms
Cancer Cell, 28(1), 15-28 (2015)
PDGFRB mutation and tyrosine kinase inhibitor resistance in Ph-like acute lymphoblastic leukemia
Blood, 131(20), 2256-2261 (2018)
Ah Ram Kim et al.
Cell, 168(6), 1053-1064 (2017-03-12)
Cytokines are classically thought to stimulate downstream signaling pathways through monotonic activation of receptors. We describe a severe anemia resulting from a homozygous mutation (R150Q) in the cytokine erythropoietin (EPO). Surprisingly, the EPO R150Q mutant shows only a mild reduction
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