- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 1332881-26-1] Sabizabulin
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-120599 |
| Brand: | MCE |
| CAS: | 1332881-26-1 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 377.39 |
| Molecular Formula | C21H19N3O4 |
| SMILES | O=C(C1=CNC(C2=CNC3=C2C=CC=C3)=N1)C4=CC(OC)=C(OC)C(OC)=C4 |
Summary
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC 50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer [1] [2] [3] .
IC50 & Target
tubulin [1]
In Vitro
VERU-111 (2.5-80 nM; 24-48 hours) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner (24 hours: IC
50
s of 25, 35 and 35 nM, respectively; 48 hours: IC
50
s of 11.8, 15.5, and 25 nM, respectively)
[4]
.
VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner
[4]
.
VERU-111 (5-20 nM; 24 hours) shows dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9, induces the expression of Bax and Bad, and inhibits the expression of Bcl-2 and Bcl-xl proteins in both AsPC-1 and Panc-1 cells
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [4]
| Cell Line: | Panc-1, AsPC-1, HPAF-II cells |
| Concentration: | 2.5, 5, 10, 20, 40, 80 nM |
| Incubation Time: | 24, 48 hours |
| Result: | Inhibited the growth of PanCa cells in a dose and time-dependent manner. The IC 50 of VERU-111 was 25, 35 and 35 nM in Panc-1, AsPC-1 and HPAF-II, respectively after 24 h treatment, while 48 h post-treatment it was 11.8, 15.5, and 25 nM. |
Apoptosis Analysis [4]
| Cell Line: | Panc-1, AsPC-1 cells |
| Concentration: | 5, 10, 20 nM |
| Incubation Time: | 24 hours |
| Result: | Arrested Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner. |
Western Blot Analysis [4]
| Cell Line: | AsPC-1 and Panc-1 cells |
| Concentration: | 5, 10, 20 nM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9 in both AsPC-1 and Panc-1 cells. Induces the expression of Bax and Bad and inhibited the expression of Bcl-2 and Bcl-xl proteins. |
In Vivo
VERU-111 (50 μg/mouse; intra-tumorally; 3 times per week for 3 weeks) effectively inhibits tumor growth as compared to vehicle-treated group. None of the mouse showed any apparent toxicity as constant increase of body weight in VERU-111 treated mice [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Six-week-old female athymic nude mice (bearing AsPC-1 cells) |
| Dosage: | 50 μg/mouse |
| Administration: | Intra-tumorally; 3 times per week for 3 weeks |
| Result: | Effectively inhibited tumor growth. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04388826 | Veru Inc. |
Respiratory Distress Syndrome, Adult
|
June 18, 2020 | Phase 2 |
| NCT04844749 | Veru Inc. |
Metastatic Castration-resistant Prostate Cancer|Androgen Resistant Prostatic Cancer
|
June 24, 2021 | Phase 3 |
| NCT05008510 | Veru Inc. |
Metastatic Triple Negative Breast Cancer
|
December 30, 2021 | Phase 2 |
| NCT05079360 | Veru Inc. |
Metastatic Breast Cancer
|
December 15, 2022 | Phase 2 |
| NCT03752099 | Veru Inc. |
Metastatic Castration Resistant Prostate Cancer
|
January 18, 2019 | Phase 1|Phase 2 |
| NCT04842747 | Veru Inc. |
SARS-CoV Infection
|
May 18, 2021 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 20 mg/mL ( 53.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6498 mL | 13.2489 mL | 26.4978 mL |
| 5 mM | 0.5300 mL | 2.6498 mL | 5.2996 mL |
| 10 mM | 0.2650 mL | 1.3249 mL | 2.6498 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (5.30 mM); Suspended solution; Need ultrasonic
References
- [1] Wang Q, et al. Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin. J Med Chem. 2019 Jul 12.
- [2] Qinghui Wang, et al. Discovery of ABI-231 analogs targeting the colchicine site in tubulin for advanced melanoma. Cancer Research 76(14 Supplement):4848-4848.
- [3] Vivek Kashyap, et al. ABI-231: A novel small molecule suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting Human papilloma virus (HPV) E6 and E7. Cancer Research 78(13 Supplement):679-679.
- [4] Kashyap VK, et al. Therapeutic efficacy of a novel βIII/βIV-tubulin inhibitor (VERU-111) in pancreatic cancer. J Exp Clin Cancer Res. 2019 Jan 23;38(1):29.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.