- ￥594 - 4650
- MedChemExpress(MCE)
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- 2025年12月05日
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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
898280-07-4
- 规格：
1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 1 mg | 产品价格： | ￥594.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1209.0 |
| 规格： | 10 mg | 产品价格： | ￥1674.0 |
| 规格： | 25 mg | 产品价格： | ￥3063.0 |
| 规格： | 50 mg | 产品价格： | ￥4650.0 |
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XL228
CAS No. : 898280-07-4
MCE 国际站：XL228
产品活性：XL228是多靶点的酪氨酸激酶抑制剂，对Bcr-Abl，Aurora A，IGF-1R，Src 和 Lyn 的IC50 值分别为5，3.1，1.6，6.1，2 nM。
研究领域：Cell Cycle/DNA Damage | Epigenetics | Protein Tyrosine Kinase/RTK
作用靶点：Aurora Kinase | Bcr-Abl | IGF-1R | Src
In Vitro: XL228 shows a broad pattern of protein kinase inhibition, including the tyrosine kinases IGF1R, SRC, ABL, FGFR1-3, and ALK and the serine/threonine kinases Aurora A and Aurora B. A panel of kinase inhibitors including XL228 is profiled against a series of cancer cell lines with known alterations in major signaling pathways. Approximately 30% of the lines demonstrate XL228 IC50 values of <100nM in viability assays, including many lines with characterized ALK or FGFR mutations or amplifications. XL228 eliminates the phosphorylation of Aurora A and B at concentrations above 10 nM. Short-term treatment of HeLa cells leads to disruption of mitotic spindle formation, with the majority of mitotic cells exhibiting a unipolar spindle and disorganized chromosomes. It displays low nanomolar biochemical activity against wild type Abl kinase (Ki=5 nM), as well as the T315I form of Abl resistant to imatinib and dasatinib (Ki=1.4 nM). XL228 inhibits phosphorylation of BCR-ABL and its substrate STAT5 in K562 cells in vitro with IC50s of 33 and 43 nM, respectively.
In Vivo: Single-dose pharmacodynamics studies demonstrate a potent effect of XL228 on BCR-ABL signaling in K562 xenograft tumors. Phosphorylation of BCR-ABL is decreased by 50% at XL228 plasma concentrations of 3.5 μM; a similar decrease in phospho-STAT5 occurred at 0.8 μM plasma concentration.
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文献和实验毛细胞白血病的治疗： （1）脾切除术：由于脾脏是毛细胞的主要来源，因此切除脾是有效的治疗方法，切脾后可迅速改善血象和全身情况，故为本病首选治疗。 （2）α-干扰素：有报道采用人类淋巴母细胞干扰素治疗17例毛细胞白血病，剂量为3xl07单位/天，或6X107单位隔日肌注，疗程4～24周。所有病例用药后2～14周，血中毛细胞消失，血红蛋白和血小板升高，14例中性粒细胞增多，2例脾脏缩小至不能扪及，因此干扰素可能成为无脾脏肿大和脾切除术后复发的首选治疗，此疗法毒性作用不明
43 13 33 46 18 107 体量（克） 1500～2500 1500～2200 223～235 动脉压毫米汞柱 107±1.4 94±2 97±1.6 79±5 140±3 135±2.3 138±3.5 145.9±0.93 心率次/分 258±2.8 270±6 258±6 291±13 181±4.3 146±2.2 228±5.4 403.5±5 血液每分流量（毫升/分） 300±70 250±10 170±30 236±13 - 218±18 56.2±
269-271 0.5 2.77 (2)3.86( β-COOH ) L- 瓜氨酸 L-citrulline(Cit) 175.19 234-237d 易溶 (3)9.82(NH 2 ) L- 半胱氨酸 L- cysteine(Cys) 121.15 易溶 5.07 (1)1.71 (2)8.33(NH 2 ) (3)10.78(SH
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