FLT3-IN-3
作者：齊岳
發(fā)布時間：2023-08-23
09:15:54
點擊數(shù)：
產(chǎn)品名稱：FLT3-IN-3
產(chǎn)品描述：
| 產(chǎn)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. |
| 靶點活性 | FLT3 (WT):13 nM, FLT3 (D835Y):8 nM |
| 體外活性 | 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. |
| 體內(nèi)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 |
存儲
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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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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