CHZ868
- Product Name
- CHZ868
- CAS No.
- 1895895-38-1
- Chemical Name
- CHZ868
- Synonyms
- CHZ868;CHZ 868; CHZ-868;CHZ868, 10 mM in DMSO;Acetamide, N-[4-[[2-[(2,4-difluorophenyl)amino]-1,4-dimethyl-1H-benzimidazol-5-yl]oxy]-2-pyridinyl]-;N-(4-((2-((2,4-Difluorophenyl)amino)-1,4-dimethyl-1H-benzo[d]imidazol-5-yl)oxy)pyridin-2-yl)acetamide
- CBNumber
- CB13133748
- Molecular Formula
- C22H19F2N5O2
- Formula Weight
- 423.42
- MOL File
- 1895895-38-1.mol
CHZ868 Property
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);236.17(Max Conc. mM)
- form
- Solid
- pka
- 13.27±0.70(Predicted)
- color
- White to gray
N-Bromosuccinimide Price
- Product number
- CS-6363
- Product name
- CHZ868
- Purity
- 99.22%
- Packaging
- 5mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- CS-6363
- Product name
- CHZ868
- Purity
- 99.22%
- Packaging
- 10mg
- Price
- $228
- Updated
- 2021/12/16
- Product number
- B5980
- Product name
- CHZ868
- Packaging
- 10mg
- Price
- $288
- Updated
- 2021/12/16
- Product number
- CS-6363
- Product name
- CHZ868
- Purity
- 99.22%
- Packaging
- 25mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- B5980
- Product name
- CHZ868
- Packaging
- 25mg
- Price
- $492
- Updated
- 2021/12/16
CHZ868 Chemical Properties,Usage,Production
Definition
ChEBI: CHZ868 is a memger of the class of benzimidazoles that is benzimidazole that is substituted by methyl groups at positions 1 and 4, by a 2,4-difluoroanilino group at position 2, and by a (2-acetamidopyridin-4-yl)oxy group at position 5. It is a type II JAK2 inhibitor with antineoplastic activity. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a member of benzimidazoles, a member of acetamides, a member of pyridines, a difluorobenzene, an aromatic ether, a secondary amino compound and an aromatic amine.
Biological Activity
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 th at 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 Preparation Products And Raw materials
Raw materials
Preparation Products
CHZ868 Suppliers
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- QQ 3285589261
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