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 | 1mg |
| CAS | 1415560-69-8 |
| 別名 | N/A |
| 化學名 | (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine hydrochloride |
| 分子式 | C21H23Cl3FN5O |
| 分子量 | 486.8 |
| 溶解度 | ≥ 100.4 mg/mL in DMSO, ≥ 101.4 mg/mL in EtOH, ≥ 52.2 mg/mL in H2O |
| 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：
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition[1][2][3].
PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively[1].
PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells[2].
PF-2341066 reveals the ability to cause marked regression of large established tumors (> 600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule in the GTL-16 model. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. A significant dose-dependent reduction of CD31-positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066[1].
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者：上海莼試生物技術有限公司
留言注意事項：
1.遵守中華人民共和國有關法律、法規，尊重網上道德，承擔一切因您的行為而直接或間接引起的法律責任。
2.請您真實的反映產品的情況,不要捏造、誣蔑、造謠。如對產品有任何疑問,也可以留言咨詢。
3.未經本站同意，任何人不得利用本留言簿發布個人或團體的具有廣告性質的信息或類似言論。
| 您感興趣的產品* | |
| 您的單位* | |
| 聯系人* | |
| 聯系電話* | |
| 詳細地址* | |
| 常用郵箱* | |
| 請輸入您對我們的意見或建議* | |
| 驗證碼* | |
 |
產品訂購說明:
1、報價含普票、運費。
2、常用試劑備貨充足，除對溫度要求極其嚴格的產品當天可發貨。
3、進口原裝產品要3-6周的貨期，詳細情況請咨詢客服。
4、訂貨時間為工作日每周一至周五16:00之前。
5、如需代為檢測，標本對環境溫度高，可聯系客服安排專人取樣（限省內客戶）。
6、代測免收代測費，一周出結果。
7、產品因運輸途中包裝破損請拒絕簽收，做退回。我們將在24小時之內為您補發 損壞產品。
8、如因單位財務制度原因，可申請先發貨，報賬后付款（此條款僅限醫院、學校信譽良好客戶）。
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
關于莼試
產品訂購
新手指南
幫助中心