Auristatin F - CAS 163768-50-1

Auristatin F - CAS 163768-50-1 Catalog number: BADC-00045

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

General Information

Category
ADCs Cytotoxin
Product Name
Auristatin F
CAS
163768-50-1
Catalog Number
BADC-00045
Molecular Formula
C40H67N5O8
Molecular Weight
745.99

Chemical Structure

  • Auristatin F

Ordering Information

Catalog Number Size Price Stock Quantity
BADC-00045 25 mg $990 In stock
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Purity
≥97.0% (HPLC)
Appearance
White to off-white solid
Synonyms
Auristatin F
Solubility
Soluble in DMSO, not in water
Storage
Dry, dark and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Application
ADCs Cytotoxin
Shipping
Room temperature
Canonical SMILES
CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)N(C)C
InChI Key
LGNCNVVZCUVPOT-FUVGGWJZSA-N
InChI
InChI=1S/C40H67N5O8/c1-13-26(6)35(44(10)39(49)33(24(2)3)42-38(48)34(25(4)5)43(8)9)31(52-11)23-32(46)45-21-17-20-30(45)36(53-12)27(7)37(47)41-29(40(50)51)22-28-18-15-14-16-19-28/h14-16,18-19,24-27,29-31,33-36H,13,17,20-23H2,1-12H3,(H,41,47)(H,42,48)(H,50,51)/t26-,27+,29-,30-,31+,33-,34-,35-,36+/m0/s1
1.An anti-HER2 antibody conjugated with monomethyl auristatin E is highly effective in HER2-positive human gastric cancer.
Li H1, Yu C2, Jiang J3, Huang C2, Yao X1, Xu Q2, Yu F2, Lou L4, Fang J1,5,6. Cancer Biol Ther. 2016 Apr 2;17(4):346-54. doi: 10.1080/15384047.2016.1139248. Epub 2016 Feb 6.
Antibody-drug conjugate (ADC) is a novel class of therapeutics for cancer target therapy. This study assessed antitumor activity of ADC with an antimitotic agent, monomethyl auristatin E (MMAE) and a humanized monoclonal anti-HER2 antibody, hertuzumab, in gastric cancer. The efficacy of hertuzumab-MC-Val-Cit-PAB-MMAE (hertuzumab-vcMMAE) on human epidermal growth factor receptor 2 (HER2) positive human gastric cancer cells, NCI-N87, was evaluated in vitro and in vivo. The cytotoxicity of hertuzumab was significantly enhanced after conjugation with MMAE. Compared to trastuzumab, hertuzumab had a higher affinity to HER2 and had more potent antibody-dependent cell-mediated cytotoxicity (ADCC) activity in vitro. After conjugation with MMAE, the binding specificity for HER2 was not affected. Furthermore, the internalization of hertuzumab-vcMMAE in HER2 positive gastric cancer cells was verified. Although the conjugation of hertuzumab and MMAE decreased the ADCC effect, the overall cytotoxicity was dramatically increased in HER2 positive gastric cancer cells.

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Historical Records: Azido-PEG4-C2-acid | Songorine | Glucopiericidin A | (2,5-dioxopyrrolidin-1-yl) 4-(methyldisulfanyl)pentanoate | Auristatin E | PF-06380101 | Nudicauline Perchlorate | m-PEG2-NHS ester | BCN-PEG4-OH | Methyltetrazine-PEG4-hydrazone-DBCO | Auristatin F
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