CHR-6494
- CAS No.
- 1333377-65-3
- Chemical Name:
- CHR-6494
- Synonyms
- 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
- Molecular Formula:
- C16H16N6
- Molecular Weight:
- 292.34
- MDL Number:
- MFCD22666352
- MOL File:
- 1333377-65-3.mol
- MSDS File:
- SDS
CHR-6494 price More Price(24)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML0648 | CHR-6494 trifluoroacetate salt ≥98% (HPLC) | 1333377-65-3 | 5mg | $123 | 2024-03-01 | Buy |
Sigma-Aldrich | 372040 | Haspin Kinase Inhibitor, CHR-6494 | 1333377-65-3 | 10mg | $259 | 2024-03-01 | Buy |
Cayman Chemical | 11478 | CHR-6494 ≥98% | 1333377-65-3 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 11478 | CHR-6494 ≥98% | 1333377-65-3 | 5mg | $93 | 2024-03-01 | Buy |
Sigma-Aldrich | SML0648 | CHR-6494 trifluoroacetate salt ≥98% (HPLC) | 1333377-65-3 | 25mg | $470 | 2023-01-07 | Buy |
CHR-6494 Chemical Properties,Uses,Production
Description
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.
Uses
CHR6494 is a small-molecule inhibitor of histone kinase haspin, with a wide spectrum of anticancer effects.
General Description
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 Preparation Products And Raw materials
Raw materials
Preparation Products
CHR-6494 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
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-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 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 |