1. Cell Cycle/DNA Damage
    Cytoskeleton
    Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin
    ADC Cytotoxin

PF-06380101 

Cat. No.: HY-12522 Purity: 99.68%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
PF-06380101 Chemical Structure

PF-06380101 Chemical Structure

CAS No. : 1436391-86-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $2452 In-stock
1 mg $880 In-stock
5 mg $1500 In-stock
10 mg $2800 In-stock
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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) [1] 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.

References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

743.01

Formula

C₃₉H₆₂N₆O₆S

CAS No.

1436391-86-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 65 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
PF-06380101
Cat. No.:
HY-12522
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