TD-106-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETD-106Cat. No.: HY-114406CAS No.: 2250288-69-6分式: CHNO分量: 273.25作靶點(diǎn): Ligand for E3 Ligase作通路: PROTAC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 (457.46 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.6597 mL 18.2983 mL 36.5965 mL5 mM 0.7319 mL 3.6597 mL 7.3193 mL10 mM 0.3660 mL 1.8298 mL 3.6597 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)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液

3、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: 2.5 mg/mL (9.15 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.15 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL A

4、CTIVITY物活性 TD-106種 CRBN 蛋調(diào)節(jié)劑，可于降解靶蛋。含 TD-106 的 BRD4 PROTAC 可誘導(dǎo) BRD4 降解 1。IC50 & Target CRBN 1體外研究 TD-106 (0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 M, and 100 M; 72hours) inhibits the proliferation ofNCI-H929 myeloma cell line with an CC50of0.039M 1.TD-106 (1, 10, 100, and 1000 nM) induces the degrad

5、ation of IKZF1/3 in NCI-H929cells 1.Cell Cytotoxicity Assay 1Cell Line: NCI-H929cellsConcentration: 72hoursIncubation Time: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 M, and 100 MResult: Inhibited cell proliferation with an CC50of0.039M.體內(nèi)研究 TD-106 (50 mg/kg; intraperitoneally; q.d. for 14 days) posse

6、sses anti-myeloma activity in SCID mice withTMD-8 xenograft model.Animal Model: Female SCID (CB-17/IcrCri-scid) mice with TMD-8 xenograft model 1Dosage: 50 mg/kgAdministration: Intraperitoneally (i.p.); q.d. for 14 daysResult: Treatment inhibited tumor growth during this duration.REFERENCES1. Kim SA, et al. A novel cereblon modulator for targeted protein degradation. Eur J Med Chem. 2019 Mar 15;166:65-74.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.T