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CC-90005

رقم الكتالوجGC62612

CC-90005 هو مثبط فعال وانتقائي وفعال عن طريق الفم لبروتين كيناز C-θ (PKC-θ) ، مع IC 50 من 8 نانومتر

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CC-90005 التركيب الكيميائي

Cas No.: 1799574-70-1

الحجم السعر المخزون الكميّة
5 mg
522٫00
متوفر
10 mg
882٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of CC-90005

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1].

CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM[1].CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM[1].

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[1].CC-90005 (100 mg/kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively[1].CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and Cmax (1.18 and 1.2 μM) following oral administration (10 and 3 mg/kg) in rat and dog, respectively[1].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[1].

[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.

Chemical Properties of CC-90005

Cas No. 1799574-70-1 SDF
Formula C21H27F2N7O2 M.Wt 447.48
الذوبان DMSO : 62.5 mg/mL (139.67 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CC-90005

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2347 mL 11.1737 mL 22.3474 mL
5 mM 0.4469 mL 2.2347 mL 4.4695 mL
10 mM 0.2235 mL 1.1174 mL 2.2347 mL
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In vivo Formulation Calculator (Clear solution) of CC-90005

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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