Auristatin E - CAS 160800-57-7
  1. Home
  2. Products
  3. ADCs Cytotoxin
  4. Auristatin E

Auristatin E - CAS 160800-57-7 Catalog number: BADC-00188

* Please be kindly noted products are not for therapeutic use. We do not sell to patients.

Auristatin E is a synthetic analog of dolastatin 10. Auristatin E is a highly potent antimitotic agent.Auristatin E inhibits tubulin polymerization. Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity.

Category
ADCs Cytotoxin
Product Name
Auristatin E
CAS
160800-57-7
Catalog Number
BADC-00188
Molecular Formula
C40H69N5O7
Molecular Weight
732.01
Purity
≥96.0% (HPLC)
Auristatin E

Ordering Information

Catalog Number Size Price Quantity
BADC-00188 5 mg $939 Inquiry

Featured Recommendations

Recommended Services
ADC Linkers Development Antibody Modification and Conjugation Technologies ADC Analysis and Characterization ADC Linker and Cytotoxin Conjugations ADC Payloads Development ADC Manufacture ADC Development for Targets ADC Development Platform
Other Types of Cytotoxins
Auristatins Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Piericidins Pyrrolobenzodiazepines Traditional Cytotoxic Agents Others
Description
Auristatin E is a synthetic analog of dolastatin 10. Auristatin E is a highly potent antimitotic agent.Auristatin E inhibits tubulin polymerization. Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity.
Synonyms
Auristatin E
IUPAC Name
(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
Canonical SMILES
CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(C)C(C2=CC=CC=C2)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)N(C)C
InChI
InChI=1S/C40H69N5O7/c1-14-26(6)35(44(11)40(50)33(24(2)3)42-39(49)34(25(4)5)43(9)10)31(51-12)23-32(46)45-22-18-21-30(45)37(52-13)27(7)38(48)41-28(8)36(47)29-19-16-15-17-20-29/h15-17,19-20,24-28,30-31,33-37,47H,14,18,21-23H2,1-13H3,(H,41,48)(H,42,49)/t26-,27+,28+,30-,31+,33-,34-,35-,36+,37+/m0/s1
InChIKey
WOWDZACBATWTAU-FEFUEGSOSA-N
Density
1.1±0.1 g/cm3
Solubility
Soluble in DMSO, not in water
Flash Point
480.6±34.3 °C
Index Of Refraction
1.519
LogP
4.75
Vapor Pressure
0.0±0.3 mmHg at 25°C
Appearance
White to off-white solid
Shelf Life
≥360 days if stored properly
Shipping
Room temperature, or blue ice upon request.
Storage
Dry, dark and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Pictograms
Health Hazard
Signal Word
Danger
Boiling Point
871.0±65.0 °C at 760 mmHg
In Vivo
Two auristatin E-based albumin-binding drugs, AE-Keto-Sulf07 and AE-Ester-Sulf07 was describeed, which were designed to release the active compound at the tumor site in a pH-dependent manner. A panel of patient- and cell-derived human tumor xenograft models (melanoma A375, ovarian carcinoma A2780, non-small-cell lung cancer LXFA737 and LXFE937, and head and neck squamous cell carcinomas) were screened with starting tumor volumes in the range of either 130-150 mm3 (small tumors) or 270-380 mm3 (large tumors). Both albumin-binding prodrugs showed compelling anticancer efficacy compared to the parent drug auristatin E, inducing statistically significant long-term partial and/or complete tumor regressions. AE-Keto-Sulf07 displayed very good antitumor response over a wide dose range, 3.0-6.5 mg/kg (5-8 injections, biweekly). AE-Ester-Sulf07 was highly efficacious between 1.9 and 2.4 mg/kg (8 injections, biweekly) or at 3.8 mg/kg (4 injections, weekly), but caused cumulative skin irritation due to scratching and biting. In contrast at its MTD, auristatin E (0.3 mg/kg, 8 injections, biweekly) was only marginally active.
NCT NumberCondition Or DiseasePhaseStart DateSponsorStatus
NCT00649584Disease, HodgkinPhase 12014-12-18Seagen Inc.Terminated (Sponsor decision not to enroll cohorts of combined SGN-35 and gemcitabine therapy.)
NCT01925612Lymphoma, B-cellPhase 22018-06-21Seagen Inc.Terminated (Sponsor decision based on portfolio prioritization and changing treatment landscape in frontline DLBCL)
NCT01990534Hodgkin LymphomaPhase 42021-04-09Millennium Pharmaceuticals, Inc.Completed
NCT01777152Anaplastic Large-Cell LymphomaPhase 32021-03-22Seagen Inc.Completed
NCT01461538Acute Lymphoid LeukemiaPhase 22016-03-04Seagen Inc.Completed
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.
The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Calculate
The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Calculate

Related Products

Muscotoxin A
Muscotoxin A
(CAS: 1653999-47-3)
Luteolin 7-O-glucoside
Luteolin 7-O-glucoside
(CAS: 5373-11-5)
7-Xylosyl-10-deacetyltaxol
7-Xylosyl-10-deacetyltaxol
(CAS: 90332-63-1)
Duocarmycin DM free base
Duocarmycin DM free base
(CAS: 1116745-06-2)
Topotecan
Topotecan
(CAS: 123948-87-8)
17-AEP-GA
17-AEP-GA
(CAS: 75747-23-8)
Historical Records: Auristatin E
Why Choose BOC Sciences?

Customer Support

Providing excellent 24/7 customer service and support

Project Management

Offering 100% high-quality services at all stages

Quality Assurance

Ensuring the quality and reliability of products or services

Global Delivery

Ensuring timely delivery of products worldwide

Featured Services
cGMP Grade Products

BOC Sciences offers comprehensive services for ADC manufacturing, including antibody modification, linker chemistry, payload conjugation, and formulation development. In particular, our payload-linker customization service offers a convenient and fast raw material channel for many ADC researchers.
Site-Specific Conjugation

BOC Sciences provides one-stop site-specific conjugation services for amino acids, glycans, unnatural amino acids, and short peptide tags. In addition, cysteine conjugation, lysine conjugation, enzymatic conjugation, thio-engineered antibody can also be obtained quickly.
Linkers for Bioconjugation

BOC Sciences offers a full range of linkers, including peptide linkers, PEG linkers, click chemistry, PROTAC linkers, non-cleavable linkers, etc. We also provide custom development services for chemically labile linkers and enzymatically cleavable linkers.
ADC Targets
Questions & Comments
Verification code
Send Inquiry
Verification code
Resources & Supports
Inquiry Basket
loading Loading ......
Delete selectedGo to checkout