GDC-0339

小分子

UNII-2PRJ7DX38T | 5-Amino-N-(5-((4R,5R)-4-amino-5-fluoroazepan-1-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide | 5-amino-N-{5-[(4R,5R)-4-amino-5-fluoroazepan-1-yl]-1-methyl-1H-pyrazol-4-yl}-2-(2,6-difluorophenyl)-1,3-thiazole-

GDC-0339

G646647-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with K i s 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 In Vitro GDC-0339 is cytostatic, with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MM.1S cells Concentration: Incubation Time: 3 days Result: Inhibited cell viability. Western Blot AnalysisCell 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. 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. GDC-0339 has a half-life of t1/2=0.9 h. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse modelDosage: 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. Form:Solid IC50& Target:Ki: 0.03 nM (Pim1), 0.1 nM (Pim2), 0.02 nM (Pim3)

GDC-0339 是一种强效、口服生物利用度高、耐受性好的泛 Pim 激酶抑制剂，对 Pim1、Pim2 和 Pim3 的 K i s 分别为 0.03 nM、0.1 nM 和 0.02 nM。GDC-0339 被发现可用于治疗多发性骨髓瘤。

1428569-85-0

C20H22F3N7OS

465.50 g/mol

73603034

CN1C(=C(C=N1)NC(=O)C2=C(SC(=N2)C3=C(C=CC=C3F)F)N)N4CC[C@H]([C@@H](CC4)F)N

5-amino-N-[5-[(4R,5R)-4-amino-5-fluoroazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide

1S/C20H22F3N7OS/c1-29-20(30-7-5-10(21)13(24)6-8-30)14(9-26-29)27-18(31)16-17(25)32-19(28-16)15-11(22)3-2-4-12(15)23/h2-4,9-10,13H,5-8,24-25H2,1H3,(H,27,31)/t10-,13-/m1/s1

NHXVGMQFCYBLTL-ZWNOBZJWSA-N

CN1C(=C(C=N1)NC(=O)C2=C(SC(=N2)C3=C(C=CC=C3F)F)N)N4CCC(C(CC4)F)N

73603034

1428569-85-0

DMSO : ≥ 52 mg/mL (111.71 mM)

3

10

4

465.156 Da

465.156 Da

143.000 Ų

32

0

657

0

1

3