CHR-6494
- Product Name
- CHR-6494
- CAS No.
- 1333377-65-3
- Chemical Name
- CHR-6494
- Synonyms
- CS-609;CHR-649;CHR-6494;CHR 6494;CHR6494;CHR-6494 trifluoroacetate salt;CHR 6494 trifluoroacetate salt;Haspin Kinase Inhibitor, CHR-6494;3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine;Imidazo[1,2-b]pyridazin-6-amine, 3-(1H-indazol-5-yl)-N-propyl-;Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem
- CBNumber
- CB92627688
- Molecular Formula
- C16H16N6
- Formula Weight
- 292.34
- MOL File
- 1333377-65-3.mol
CHR-6494 Property
- Density
- 1.39±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble5mg/mL, clear (warmed)
- pka
- 13.24±0.40(Predicted)
- form
- powder
- color
- white to beige
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0648
- Product name
- CHR-6494 trifluoroacetate salt
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $123
- Updated
- 2024/03/01
- Product number
- 372040
- Product name
- Haspin Kinase Inhibitor, CHR-6494
- Packaging
- 10mg
- Price
- $259
- Updated
- 2024/03/01
- Product number
- 11478
- Product name
- CHR-6494
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 11478
- Product name
- CHR-6494
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- SML0648
- Product name
- CHR-6494 trifluoroacetate salt
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $470
- Updated
- 2023/01/07
CHR-6494 Chemical Properties,Usage,Production
Description
CHR-6494 is a haspin protein kinase inhibitor (IC50 = 2 nM) selective over 27 other protein kinases, including Aurora B kinase (IC50 > 1 μM). Haspin is a kinase necessary for mitosis that selectively phosphorylates histone 3 at the threonine 3 residue (H3T3ph). CHR-6494 decreases phosphorylation of H3T3 and arrests the cell cycle in the G2/M phase, which leads to apoptosis. It showed promising results in a xenograft tumor model.
Uses
CHR6494 is a small-molecule inhibitor of histone kinase haspin, with a wide spectrum of anticancer effects.
General Description
A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2 nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100 nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752 nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1 μM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50 mg/kg, i.p.).
CHR-6494 Preparation Products And Raw materials
Raw materials
Preparation Products
CHR-6494 Suppliers
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- 021-58955995
- Fax
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- Country
- United States
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