CHR-6494
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CHR-6494 속성
- 밀도
- 1.39±0.1 g/cm3(Predicted)
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 용해성5mg/mL, 투명(가온)
- 산도 계수 (pKa)
- 13.24±0.40(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
안전
| WGK 독일 | 3 |
|---|
CHR-6494 C화학적 특성, 용도, 생산
개요
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.일반 설명
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 준비 용품 및 원자재
원자재
준비 용품
CHR-6494 공급 업체
글로벌( 70)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| 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 | +1-833-552-7181 |
sales@aladdinsci.com | United States | 52927 | 58 |
| Amadis Chemical Company Limited | 571-89925085 |
sales@amadischem.com | China | 131981 | 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 |