TAS6417 - EGFR 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETAS6417Cat. No.: HY-112299CAS No.: 1661854-97-2分式: CHNO分量: 396.44作靶點(diǎn): EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (315.

2、31 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5224 mL 12.6122 mL 25.2245 mL5 mM 0.5045 mL 2.5224 mL 5.0449 mL10 mM 0.2522 mL 1.2612 mL 2.5224 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠

3、性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (5.68 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (5.68 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn

4、 oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.25 mg/mL (5.68 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TAS6417表長(zhǎng)因受體 (EGFR) 的抑制劑，也 治療細(xì)胞肺癌的有效候選藥物，其 IC50 值為 1.1-8.0 nM。IC50 & Target EGFR1.1-8.0 nM (IC50)體外研究 TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mut

5、ants including an exon 20 insertionmutation, with IC50 values ranging from 1.10.1 to 8.01.1 nM. TAS6417 suppresses the growth of cellsexpressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.528.5 nM for LXF 2478Lcells and 45.42.6 nM for NCI-H1975 EGFR D770_N771insSVD cells.

6、TAS6417 also potently inhibitsproliferation in other cell lines harboring activating mutations or acquired resistance mutations, with meanGI50 values of 1.920.21 nM to 7.120.60 nM. In contrast, the effect of TAS6417 on cell proliferation innormal human epidermal keratinocytes (NHEK-Neo), of which WT

7、 EGFR is implicates in the growth andsurvival, is moderate 1.體內(nèi)研究 TAS6417 causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models.TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. TAS6417 prolongs survival ofanimals bearing lung cancer 1.PROTOCO

8、LAnimal Mice 1Mice bearing NCI-H1975 EGFR D770_N771insSVD xenografts are orally administered TAS6417 (50,Administration 1 100, 200 mg/kg). One and 2 hours after administration of TAS6417, xenograft tumors and skin tissues arecollected 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658.McePdfHeightCaution: Product has not been fully validated for medical app