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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity
In Vitro
CCR4-351 (compound 38) hydrochloride shows no activity in a CYP450 induction assay. CCR4-351 hydrochloride inhibits the migration of mouse iT reg cells with an IC 50 of 39 nM, while the IC 50 in human iT reg cells is 33 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) hydrochloride significantly reduces the tumor growth . CCR4-351 (0.5 mg/kg; IV) hydrochloride has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V ss =5.2 L/kg), a T 1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse . CCR4-351 hydrochloride has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 hydrochloride has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor Dosage: 50 mg/kg Administration: PO; daily; for 40 days Result: Significantly reduced the tumor growth. Animal Model: Rat and mouse Dosage: 0.5 mg/kg of IV; 2 mg/kg of PO Administration: IV or PO Result: Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat. Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V ss =5.2 L/kg), a T 1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
Form:Solid
IC50& Target:CCR4
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | DMSO : 170 mg/mL (Need ultrasonic) |
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