Successful, we will reply to you quickly.

OK

Please select the quantity.

OK

Your message is being sent, please wait.

Close

test

Close

Send mail failed, please send again!

Close

Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

PF-06380101

HY-12522

PF-06380101

PF-06380101 Chemical Structure

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.

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
Size Price Stock Quantity
10 mM * 1 mL in DMSO €2403 In-stock
1 mg €862 In-stock
5 mg €1470 In-stock
10 mg €2744 In-stock
50 mg Get quote
100 mg Get quote

* Please select Quantity before adding items.

Bulk Inquiry

Inquiry Information
Product name: PF-06380101
Cat. No.: HY-12522

PF-06380101 Data Sheet

  • View current batch:

    Purity: 99.68%

  • Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

    Pdf Version

    NMR

    Pdf Version

    HPLC

    Pdf Version

    LCMS

Related Compound Libraries

Biological Activity of PF-06380101

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.

Protocol (Extracted from published papers and Only for reference)

More

Chemical Information

M.Wt 743.01 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₃₉H₆₂N₆O₆S
CAS No 1436391-86-4
Solvent & Solubility

DMSO: ≥ 65 mg/mL

Preparing Stock Solutions

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

References on PF-06380101

Inhibitor Kit
  • 10-Deacetyl-7-xylosyl paclitaxel

    10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.

  • 10-Oxo Docetaxel

    10-Oxo Docetaxel(Docetaxel Impurity) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.

  • 2-Methoxyestradiol

    2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 (plusmn) 0.11 (mu)M for the inhibition of BPAEC migration.

  • 4'-Demethylepipodophyllotoxin

    4(acute)-Demethylepipodophyllotoxin(4(acute)-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.

  • 7-Epi-10-oxo-docetaxel

    7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).

  • 7-Epi-docetaxel

    7-Epi-10-oxo-docetaxel (Docetaxel Impurity C; 7-Epitaxotere) is a impurity of docetaxel.

  • 7-xylosyltaxol

    7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) derivative; Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.

  • ABT-751

    ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 (mu)M in neuroblastoma and non-neuroblastoma cell lines, respectively.

  • alpha-Amanitin

    alpha-Amanitin is a potent inhibitor of DNA-dependent RNA polymerase II.

  • Auristatin E

    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.

MORE