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PF-06380101 Chemical Structure
|Product name: PF-06380101|
|Cat. No.: HY-12522|
PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) 
Target: ADCs cytotoxin; tubulin inhibitor
After an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9,CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
|M.Wt||743.01||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 65 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.3459 mL||6.7294 mL||13.4588 mL|
|5 mM||0.2692 mL||1.3459 mL||2.6918 mL|
|10 mM||0.1346 mL||0.6729 mL||1.3459 mL|
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