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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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CHR-6494 Suppliers

China 62 United Kingdom 1 United States 14 Global 77
Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58

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