3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt
CHR-6494
CAS: 1333377-65-3
Molecular Formula: C16H16N6
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt - Names and Identifiers
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt - Physico-chemical Properties
| Molecular Formula | C16H16N6 |
| Molar Mass | 292.34 |
| Density | 1.39±0.1 g/cm3(Predicted) |
| Solubility | DMSO: soluble5mg/mL, clear (warmed) |
| Appearance | powder |
| Color | white to beige |
| pKa | 13.24±0.40(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | CHR-6494 is a potent inhibitor of haspin, inhibiting histone H3T3 phosphorylation, with an IC 50 of 2 nM. CHR-6494 does not modify H3S10 and H328 phosphorylation levels, and shows no significantly inhibitory effects on other protein kinases such as Aurora B kinase. CHR-6494 dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cell, with IC 50 s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively. CHR-6494 (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. CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC 50 s ranging from 396 nM to 1229 nM. CHR-6494 (300 nM and 600 nM) 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 cells. CHR-6494 in combination with MEK inhibitors synergistically inhibits viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells. |
| In vivo study | CHR-6494 (50 mg/kg, i.p.) inhibits the growth of tumor and cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells. |
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt - Risk and Safety
| WGK Germany | 3 |
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.421 ml | 17.103 ml | 34.207 ml |
| 5 mM | 0.684 ml | 3.421 ml | 6.841 ml |
| 10 mM | 0.342 ml | 1.71 ml | 3.421 ml |
| 5 mM | 0.068 ml | 0.342 ml | 0.684 ml |
Last Update：2024-01-02 23:10:35
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt - Reference Information
| biological activity | CHR-6494 is an effective haspin inhibitor, which can inhibit the phosphorylation of histone H3T3 with an IC50 value of 2 nM. |
| target | IC50: 2 nM (haspin) |
| in vitro study | CHR-6494 is a potent inhibitor of haspin, inhibiting histone H3T3 phosphorylation, with an IC 50 of 2 nM. CHR-6494 does not modify H3S10 and H328 phosphorylation levels, and shows no significantly inhibitory effects on other protein kinases such as Aurora B kinase. CHR-6494 dose-dependently inhibits the growth of cancer cells, such as HCT-116, heLa, MDA-MB-231, and Wi-38 cell, with IC 50 s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively. CHR-6494 (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. CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC 50 s ranging from 396 nM to 1229 nM. CHR-6494 (300 nM and 600 nM) 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 cells. CHR-6494 in combination with MEK inhibitors synergistically inhibits viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells. |
| in vivo study | CHR-6494 (50 mg/kg, I. p.) inhibits the growth of tumor and cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells. |
Last Update：2024-04-09 02:00:01
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Spot supply
Product Name: CHR-6494 Visit Supplier Webpage Request for quotationCAS: 1333377-65-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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