13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 25mg 100mg 500mg 1g |
| CAS | 950769-58-1 |
| 別名 | N/A |
| 化學名 | 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea |
| 分子式 | C29H32N6O4S |
| 分子量 | 560.67 |
| 溶解度 | ≥ 28.0335mg/mL in DMSO |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
Quizartinib (AC220) is a 2nd-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 value of 1.1 nM/4.2 nM, and it is ten-fold more selective for Flt3 than PDGFRα, PDGFRβ, KIT, RET and CSF-1R [1].
Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and shows high selectivity when screened against most of the human protein kinome. In addition, the combination of high potency and selectivity exhibited by quizartinib is unique compared with CEP-701, PKC-412, MLN-518, sunitinib, and sorafenib.
Quizartinib (AC220) was identified to be the most potent and selective FLT3 inhibitor with good pharmaceutical properties and superior efficacy in tumor xenograft models. A single dose of 10 mg/kg was administered to mice by oral gavage and plasma levels were measured over a 24-hour period. Quizartinib was well absorbed, achieving a maximum plasma level (Cmax) of 3.8 μM (2100 ng/mL) within 2 hours of dosing. To determine the effect of FLT3-ITD inhibition on cell growth,. These results establish that AC220 has strong activity against FLT3 in biochemical and cellular assays in MV4-11 cell proliferation in the presence of 1.1nM quizartinib [1].
As a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML), when at doses as low as 1 mg/kg orally once a day, quizartinib inhibits FLT3 activity in vivo extending survival significantly. And this eradicates tumors in a FLT3-dependent mouse xenograft model, and potently inhibits FLT3 activity in primary patient cells at a dose of 10 mg/kg. In addition, quizartinib has been demonstrated a desirable safety and PK profile in humans. The emergence of resistant mutations is a common mechanism of resistance to FLT3 inhibitors used clinically, with a mutation emerging in at least 20% of the patients. This shows that the survival of AML blasts depends to a great extent on FLT3 signaling in these cases [2, 3].
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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