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CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM).
CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 1,300 | 5日内发货 | |
5 mg | ¥ 2,190 | 5日内发货 | |
25 mg | ¥ 5,940 | 6-8周 | |
50 mg | ¥ 7,720 | 6-8周 | |
100 mg | ¥ 11,900 | 6-8周 | |
1 mL x 10 mM (in DMSO) | ¥ 2,250 | 5日内发货 |
产品描述 | CAL-130 Hydrochloride is a PI3Kδ and PI3Kγ inhibitor (IC50s: 1.3 and 6.1 nM). |
靶点活性 | p110β:56 nM, p110δ:1.3 nM, p110α:115 nM, p110γ:6.1 nM |
体外活性 | CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains (IC50s: 1.3 and 6.1 nM for p110δ and p110γ, 115 and 56 nM for p110α and p110β). CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival. |
体内活性 | The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Ptenfl/fl mice with established T cell acute lymphoblastic leukemia. Candidate animals for survival studies are ill-appearing, have a white blood cell count above 45,000/μL, evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double-positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared to 7.5 days for the control group. |
分子量 | 462.94 |
分子式 | C23H23ClN8O |
CAS No. | 1431697-78-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (108.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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