FLT3-IN-3
作者：齐岳
发布时间：2023-08-23
09:15:54
点击数：
产品名称：FLT3-IN-3
产品描述：
| 产品描述 | FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively. |
| 靶点活性 | FLT3 (WT):13 nM, FLT3 (D835Y):8 nM |
| 体外活性 | FLT3-IN-3 ?inhibits the proliferation of FLT3-ITD positive MV4-11 and MOLM-13 cell lines very effectively at low nanomolar concentrations (GI50 values 2 and 1 nM, respectively).?FLT3-IN-3 (1 nM, 10nM, 100 nM, 1 μM and 10 μM;?72 hours) inhibits the Ba/F3 FLT3-ITD cells with the GI50 of 0.034±0.015 μM, and inhibits the parental Ba/F3 cells with the GI50 value of 1.136±0.389 μM.?Concentrations as low as 1 nM are sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842).?Moreover, this inhibition suppresses phosphorylation of several downstream targets of FLT3.?Notably, FLT3-IN-3 (0.01, 0.1, 1, 10 and 100 nM;?1 hours) abolishes phosphorylation of STAT5 at Y694, which is a direct substrate of the oncogenic FLT3-ITD variant.?The second pathway affected is the MAPK cascade: Two key components of this signaling pathway, ERK1/2 (T202/Y204) and MEK1/2 (S217/221), exhibit reduced phosphorylation upon treatment with FLT3-IN-3.?FLT3-IN-3 also interfers with PI3K/AKT pathway which is confirmed by reduced phosphorylation of AKT at S473. |
| 体内活性 | A single dose of FLT3-IN-3 ?in mice with subcutaneous MV4-11 xenografts causes sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours. |
| 分子量 | 490.64 |
| 分子式 | C27H38N8O |
| CAS No. | 2229050-90-0 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 250 mg/mL (509.54 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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