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SML3399

Sigma-Aldrich

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:
1895895-38-1
Molecular Weight:
423.42
MDL number:
MFCD30533612
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to pink

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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)
PDGFRB mutation and tyrosine kinase inhibitor resistance in Ph-like acute lymphoblastic leukemia
Blood, 131(20), 2256-2261 (2018)
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)
Shuo-Chieh Wu et al.
Cancer cell, 28(1), 29-41 (2015-07-16)
A variety of cancers depend on JAK2 signaling, including the high-risk subset of B cell acute lymphoblastic leukemias (B-ALLs) with CRLF2 rearrangements. Type I JAK2 inhibitors induce paradoxical JAK2 hyperphosphorylation in these leukemias and have limited activity. To improve the
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