MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

FLT3-IN-3

產(chǎn)品活性：FLT3-IN-3 是一種有效的 FLT3 抑制劑，抑制 FLT3 WT 和 FLT3 D835Y，IC₅₀ 分別為 13 和 8 nM。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK

作用靶點(diǎn)：FLT3

In Vitro: FLT3-IN-3 (Compound 7d) 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.

In Vivo: A single dose of FLT3-IN-3 (Compound 7d; 10 mg/kg; i.p.) in mice with subcutaneous MV4-11 xenografts causes sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Membrane Protein-targeted Compound Library  |  JNJ-47117096 hydrochloride  |  Sorafenib-d₄  |  AT9283  |  (E/Z)-Zotiraciclib  |  AKN-028 acetate  |  Sorafenib Tosylate  |  BPR1K871  |  ENMD-2076 Tartrate  |  AZD2932  |  Hypothemycin  |  UNC2025 hydrochloride  |  Tandutinib  |  UNC4203  |  3-Hydroxy Midostaurin  |  Cabozantinib  |  LBW242  |  MAX-40279 hemifumarate  |  JAK2-IN-7  |  TAK-659 hydrochloride  |  Gilteritinib-d₈  |  BSc5371  |  FLT3/CDK4-IN-1  |  Tyrphostin AG1296  |  FLT3-IN-4  |  FLT3-IN-18  |  Cabozantinib-d₄  |  Gilteritinib hemifumarate  |  Tuspetinib

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動(dòng)劑涉及各熱門信號(hào)通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測(cè)分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊(duì)跟蹤新的制藥及生命科學(xué)研究進(jìn)展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機(jī)構(gòu)建立了長(zhǎng)期的合作。