CHR-6494
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406782

CAS#: 1333377-65-3

Description: CHR-6494 is a potent and selective histone kinase Haspin inhibitor. CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification. CHR-6494 shows antitumor potential in xenografted nude mice without any observed toxicity. Thus, CHR-6494 is a first-in-class Haspin inhibitor with a wide spectrum of anticancer effects that merits further preclinical research as a new member of the family of mitotic kinase inhibitors.

Chemical Structure

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CHR-6494
CAS# 1333377-65-3
Instruction

Theoretical Analysis

MedKoo Cat#: 406782
Name: CHR-6494
CAS#: 1333377-65-3
Chemical Formula: C16H16N6
Exact Mass: 292.14
Molecular Weight: 292.350
Elemental Analysis: C, 65.74; H, 5.52; N, 28.75

Price and Availability

Size Price Availability Quantity
5mg USD 285 2 Weeks
10mg USD 500 2 Weeks
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Synonym: CHR-6494; CHR 6494; CHR6494.

IUPAC/Chemical Name: 3-(1H-indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine

InChi Key: CZZCAOGIEGXMBZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H16N6/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/h3-6,8-10H,2,7H2,1H3,(H,17,21)(H,19,20)

SMILES Code: CCCNC1=NN2C(C=C1)=NC=C2C3=CC4=C(NN=C4)C=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 12.5 42.76
DMSO 20.0 68.41
Ethanol 0.3 0.86

Preparing Stock Solutions

The following data is based on the product molecular weight 292.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kang H, Park YS, Cho DH, Kim JS, Oh JS. Dynamics of histone H3 phosphorylation at threonine 3 during meiotic maturation in mouse oocytes. Biochem Biophys Res Commun. 2015 Mar 6;458(2):280-6. doi: 10.1016/j.bbrc.2015.01.099. Epub 2015 Jan 31. PubMed PMID: 25645018.

2: Huertas D, Soler M, Moreto J, Villanueva A, Martinez A, Vidal A, Charlton M, Moffat D, Patel S, McDermott J, Owen J, Brotherton D, Krige D, Cuthill S, Esteller M. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18. doi: 0.1038/onc.2011.335. Epub 2011 Aug 1. PubMed PMID: 21804608; PubMed Central PMCID: PMC3312407.