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GDC-0339

    
≥98%

GDC-0339

源葉(MedMol)
S83260 一鍵復制產品信息
1428569-85-0
C20H22F3N7OS
465.4952
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S83260-5mg
≥98% ¥6500.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma

產品描述: GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma
靶點: Ki: 0.03 nM (Pim1), 0.1 nM (Pim2), 0.02 nM (Pim3);Pim
體外研究: GDC-0339 is cytostatic, with an IC50 of 0.1 μM for MM.1S cells. GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases. Cell Viability Assay Cell Line: MM.1S cells Concentration: Incubation Time: 3 days Result: Inhibited cell viability. Western Blot Analysis Cell Line: MM.1S cells Concentration: 0.01 μM, 0.03 μM, 0.09 μM,0.27 μM, 0.83 μM, 2.5 μM Incubation Time: 4 hours Result: Induced a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.
體內研究: GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models. GDC-0339 has a half-life of t1/2=0.9 h. Animal Model: Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model Dosage: 1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg Administration: Oral administration; once daily; for 21 days Result: Showed dose-dependent tumor growth inhibition.
參考文獻: 1. Takahashi RH, et al. CYP1A1-Mediated Intramolecular Rearrangement of Aminoazepane in GDC-0339. Drug Metab Dispos. 2017 Oct;45(10):1084-1092. 2. Wang X, et al. Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. J Med Chem. 2019 Feb 28;62(4):2140-2153.
溶解性: soluble  in  DMSO
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 2.148 ml 10.741 ml 21.482 ml
5 mM 0.43 ml 2.148 ml 4.296 ml
10 mM 0.215 ml 1.074 ml 2.148 ml
50 mM 0.043 ml 0.215 ml 0.43 ml
注意: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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