CHR-6494

CHR-6494 Struktur
1333377-65-3
CAS-Nr.
1333377-65-3
Englisch Name:
CHR-6494
Synonyma:
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
Summenformel:
C16H16N6
Molgewicht:
292.34
MOL-Datei:
1333377-65-3.mol

CHR-6494 Eigenschaften

Dichte
1.39±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
Löslichkeit
DMSO: soluble5mg/mL, clear (warmed)
pka
13.24±0.40(Predicted)
Aggregatzustand
powder
Farbe
white to beige

Sicherheit

WGK Germany  3

CHR-6494 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Allgemeine Beschreibung

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


CHR-6494 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 70)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 19892 58
Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525
masar@topule.com China 8474 58
Aladdin Scientific
+1-833-552-7181
sales@aladdinsci.com United States 52927 58
Amadis Chemical Company Limited
571-89925085
sales@amadischem.com China 131981 58
Shanghai Boyle Chemical Co., Ltd.
sales@boylechem.com China 2923 55
Haoyuan Chemexpress Co., Ltd. 021-58950125
info@chemexpress.com China 7553 61
MedChemexpress LLC 021-58955995
sales@medchemexpress.cn United States 4863 58
AdooQ BioScience, LLC +1 (866) 930-6790
info@adooq.com United States 2784 58
CEG Chemical Science&Technology Co., Ltd. Mobile:13665161512
China 1785 58
Shanghai HuanChuan Industry Co.,Ltd. 021-61478794
sales@hcshhai.com China 9798 50

1333377-65-3()Verwandte Suche:


  • 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
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