CHR-6494
- Product Name
- CHR-6494
- CAS No.
- 1333377-65-3
- Chemical Name
- CHR-6494
- Synonyms
- CS-609;CHR-649;CHR-6494;CHR-6494 ，E1132;CHR 6494;CHR6494;CHR-6494, 10 mM in DMSO;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
- 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
- InChI
- 1S/C16H16N6.C2HF3O2/c1-2-7-17-15-5-6-16-18-10-14(22(16)21-15)11-3-4-13-12(8-11)9-19-20-13;3-2(4,5)1(6)7/h3-6,8-10H,2,7H2,1H3,(H,17,21)(H,19,20);(H,6,7)
- InChIKey
- ILWYDZNXJQESDI-UHFFFAOYSA-N
- SMILES
- OC(=O)C(F)(F)F.CCCNc1ccc2ncc(-c3ccc4[nH]ncc4c3)n2n1
Safety
- WGK Germany
- 3
- Storage Class
- 11 - Combustible Solids
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML0648
- Product name
- CHR-6494 trifluoroacetate salt
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $115
- Updated
- 2026/03/19
- Product number
- 372040
- Product name
- Haspin Kinase Inhibitor, CHR-6494
- Packaging
- 10mg
- Price
- $242
- Updated
- 2026/03/19
- 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.).
References
[1] D HUERTAS. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin[J]. Oncogene, 2011, 31 11: 1408-1418. DOI: 10.1038/onc.2011.335
CHR-6494 Preparation Products And Raw materials
Raw materials
Preparation Products
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