1. Cell Cycle/DNA Damage
  2. Haspin Kinase
  3. CHR-6494 TFA

CHR-6494 TFA 

Cat. No.: HY-110350
Handling Instructions

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer.

For research use only. We do not sell to patients.

CHR-6494 TFA Chemical Structure

CHR-6494 TFA Chemical Structure

CAS No. : 1458630-17-5

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Description

CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].

IC50 & Target[1]

haspin

2 nM (IC50)

In Vitro

CHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively[1].
CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay[1].
CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM[2].
CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells[1].
CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1]
Dosage: 50 mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin)
Administration: i.p. in two cycles of five consecutive days for 15 days
Result: Dose-dependent tumor growth inhibition was demonstrated.
Did not change the body weight of mice.
Animal Model: 4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors
Dosage: 20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin
Administration: i.p. for 15 consecutive days
Result: Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.
Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.
Molecular Weight

406.36

Formula

C18H17F3N6O2

CAS No.
SMILES

CCCNC1=NN2C(C3=CC4=C(C=C3)NN=C4)=CN=C2C=C1.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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CHR-6494 TFA
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