CC-90005 是一种有效，选择性和具有口服活性的蛋白激酶 C-θ (PKC-θ) 抑制剂，IC₅₀ 值为 8 nM。CC-90005 显示了对 PKC-θ 的选择性超过 PKC-δ (IC₅₀=4440 nM)。CC-90005 可以通过抑制 IL-2 表达抑制 T 细胞活化。

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC 50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC 50 =4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression.

Solid

PKCθ 8 nM (IC50)

CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM.
CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes.
CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM.
CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

CC-90005 (3-30 mg/kg; p.o. twice daily for 4 days) significantly reduces the popliteal lymph node (PLN) size in a model of chronic T cell activation.
CC-90005 (100 mg/kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively.
CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and C max (1.18 and 1.2 μM) following oral administration (10 and 3 mg/kg) in rat and dog, respectively.
CC-90005 exhibits the mean residence time (0.52 and 2.0 h), CL (69.1 and 20.5 mL/min/kg) and Vss (2.11 and 2.44 L/kg) following intravenous administration (2 and 1 mg/kg) in rat and dog, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Papa P, et, al. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005. J Med Chem. 2021 Aug 26;64(16):11886-11903.

In Vitro: DMSO : 62.5 mg/mL (139.67 mM; Need ultrasonic)配制储备液