GDC-0339 是一种高效、具有口服活性、耐受性良好的pan-Pim 激酶抑制剂，对 Pim1、Pim2 和 Pim3 作用的Ki值分别为 0.03 nM、0.1 nM 和 0.02 nM。GDC-0339 具有研究多发性骨髓瘤的潜力。
| 生物活性 | GDC-0339 is a potent, orally bioavailable and well toleratedpan-Pim kinaseinhibitor, withKis of 0.03 nM, 0.1 nM and 0.02 nM forPim1,Pim2andPim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma[1][2]. |
| IC50& Target | Ki: 0.03 nM (Pim1), 0.1 nM (Pim2), 0.02 nM (Pim3)[2] |
体外研究
(In Vitro) | GDC-0339 is cytostatic, with an IC50of 0.1 μM for MM.1S cells[2].
GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases[2].
Cell Viability Assay[2] | Cell Line: | MM.1S cells | | Concentration: | | | Incubation Time: | 3 days | | Result: | Inhibited cell viability. |
Western Blot Analysis[2] | 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. |
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体内研究
(In Vivo) | 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[2].
GDC-0339 has a half-life of t1/2=0.9 h[2].
| Animal Model: | Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 52 mg/mL(111.71 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.1482 mL | 10.7411 mL | 21.4823 mL | | 5 mM | 0.4296 mL | 2.1482 mL | 4.2965 mL | | 10 mM | 0.2148 mL | 1.0741 mL | 2.1482 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
