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372040 Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem

372040
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1333377-65-3C₁₆H₁₆N₆

Products

Catalogue NumberPackaging Qty/Pack
372040-10MG Sklená flaša 10 mg
Description
OverviewA 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.).
Catalogue Number372040
Brand Family Calbiochem®
Synonyms3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine
References
ReferencesHuertas, D., et al. 2012. Oncogene 31, 1408.
Product Information
CAS number1333377-65-3
FormOff-white solid
Hill FormulaC₁₆H₁₆N₆
Chemical formulaC₁₆H₁₆N₆
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
372040-10MG 04055977213553

Documentation

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

Title

Safety Data Sheet (SDS) 

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

TitleLot Number
372040

References

Reference overview
Huertas, D., et al. 2012. Oncogene 31, 1408.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision06-February-2013 JSW
Synonyms3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine
DescriptionA 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.).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1333377-65-3
Chemical formulaC₁₆H₁₆N₆
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesHuertas, D., et al. 2012. Oncogene 31, 1408.