CHR-6494

ChemicalBook > CAS DataBase List > 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

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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

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0648
Product name: CHR-6494 trifluoroacetate salt
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $123
Updated: 2024/03/01

Sigma-Aldrich

Product number: 372040
Product name: Haspin Kinase Inhibitor, CHR-6494
Packaging: 10mg
Price: $259
Updated: 2024/03/01

Cayman Chemical

Product number: 11478
Product name: CHR-6494
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 11478
Product name: CHR-6494
Purity: ≥98%
Packaging: 5mg
Price: $93
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0648
Product name: CHR-6494 trifluoroacetate salt
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $470
Updated: 2023/01/07

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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

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1333377-65-3, CHR-6494Related Search:

N-PROPYLBENZENE Trichloropropylsilane

3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine

CHR-6494 3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine

3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt

3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt

CHR 6494 trifluoroacetate salt

CHR-6494 trifluoroacetate salt

Haspin Kinase Inhibitor, CHR-6494

CHR-6494

CHR-649

Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem

CS-609

CHR 6494;CHR6494

Imidazo[1,2-b]pyridazin-6-amine, 3-(1H-indazol-5-yl)-N-propyl-

1333377-65-3