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[CAS NO. 1047645-82-8] Afuresertibhydrochloride
| 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-15727A |
| Brand: | MCE |
| CAS: | 1047645-82-8 |
Overview
| MDL | MFCD28167824 |
|---|---|
| Molecular Weight | 463.78 |
| Molecular Formula | C18H18Cl3FN4OS |
| SMILES | O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN.[H]Cl |
11 Publications Citing Use of MCE
- [1]Sci Transl Med. 2021 Jan 27;13(578):eaba7308.
- [2]Cell Syst. 2018 Apr 25;6(4):424-443.e7.
- [3]Theranostics. 2019 Jan 30;9(4):1096-1114.
- [4]Cancers (Basel). 2022 May 19;14(10):2493.
- [5]Int J Cancer. 2020 Apr 1;146(7):1963-1978.
- [6]Genes Dis. 2021 Aug 17;9(2):562-575.
- [7]J Physiol. 2017 Jul 1;595(13):4207-4225.
- [8]Molecules. 2019 Apr 1;24(7):1260.
- [9]Research Square Print. October 27th, 2022.
- [10]Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140.
- [11]Methods Mol Biol. 2018;1711:351-398.
Summary
IC50 & Target
|
Akt1 0.08 nM (Ki) |
Akt2 2 nM (Ki) |
Akt3 2.6 nM (Ki) |
Akt1 E17K mutant 0.2 nM (IC 50 ) |
PKCη 210 nM (IC 50 ) |
PKC-βI 430 nM (IC 50 ) |
||||
|
ROCK 100 nM (IC 50 ) |
PKCθ 510 nM (IC 50 ) |
||||||||
In Vitro
Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G
1
phase.
Western blotting analysis shows that Afuresertib increases the expression of p21
WAF1/CIP1
and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G
1
phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression
E2F1
and
MYC
, which are associated with fibroblast core serum response
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01532700 | University Health Network, Toronto|Novartis |
Chronic Lymphocytic Leukemia (CLL)
|
February 2012 | Phase 2 |
| NCT04060394 | Laekna Limited |
Metastatic Castration-resistant Prostate Cancer
|
September 13, 2019 | Phase 1|Phase 2 |
| NCT04851613 | Laekna LLC|Laekna Limited |
Breast Cancer
|
February 18, 2022 | Phase 1 |
| NCT02040480 | GlaxoSmithKline |
Cancer
|
February 5, 2014 | Phase 1 |
| NCT01476137 | GlaxoSmithKline |
Cancer
|
October 26, 2011 | Phase 1 |
| NCT01653912 | Accenture |
Recurrent Platinum-resistant Ovarian Cancer
|
November 2012 | Phase 1|Phase 2 |
| NCT02235740 | Novartis|Amgen |
Cancer
|
November 2014 | Phase 1 |
| NCT01827644 | GlaxoSmithKline |
Cancer
|
April 24, 2013 | Phase 1 |
| NCT05383482 | Laekna Limited |
Solid Tumor|NSCLC|Cervical Cancer|Endometrial Cancer|Esophageal Cancer|Gastric and Gastroesophageal Junction Adenocarcinoma
|
June 30, 2022 | Phase 1|Phase 2 |
| NCT02177682 | Novartis Pharmaceuticals|Novartis |
Neoplasms, Haematologic
|
August 13, 2014 | Phase 1 |
| NCT02240212 | Novartis Pharmaceuticals|Novartis |
Cancer
|
October 2014 | Phase 1 |
| NCT05390710 | Laekna Limited |
Solid Tumor|TNBC - Triple-Negative Breast Cancer
|
June 12, 2021 | Phase 1|Phase 2 |
| NCT02380313 | GlaxoSmithKline |
Cancer
|
October 2015 | Phase 1 |
| NCT04374630 | Laekna Limited |
Platinum-resistant Ovarian Cancer
|
June 9, 2020 | Phase 2 |
| NCT01395004 | GlaxoSmithKline |
Langerhans Cell Histiocytosis
|
November 2011 | Phase 2 |
| NCT01428492 | Novartis |
Multiple Myeloma
|
December 2011 | Phase 1 |
| NCT01531894 | Novartis Pharmaceuticals|Novartis |
Cancer
|
February 8, 2012 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 215.62 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1562 mL | 10.7810 mL | 21.5619 mL |
| 5 mM | 0.4312 mL | 2.1562 mL | 4.3124 mL |
| 10 mM | 0.2156 mL | 1.0781 mL | 2.1562 mL |
References
- [1] Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659.
- [2] Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880
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