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GSK215

GSK215 Structure
GSK215 structure
CAS No.
2743427-26-9
Chemical Name:
GSK215
Synonyms
GSK215;(2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
CBNumber:
CB810705803
Molecular Formula:
C50H59F3N10O6S
Molecular Weight:
985.14
MDL Number:
MOL File:
2743427-26-9.mol
Last updated:2024-07-02 08:55:17
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GSK215 Properties

Boiling point 1103.2±65.0 °C(Predicted)
Density 1.317±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 250 mg/mL (253.77 mM; Need ultrasonic)
form Solid
pka 13.97±0.40(Predicted)
color Off-white to light yellow
InChIKey ZGSWGXNEXAXEGV-VSAGVCMVNA-N

GSK215 Chemical Properties,Uses,Production

Biological Activity

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect[1]. GSK215 (0.1-1000 nM; 2 hours) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM[1]. GSK215 (8mg/kg; i.h.) treatment shows the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1].

in vitro

GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells. Its induced degradation is proteasome and ubiquitin-dependent. GSK215 (above 100 nM, 6h) primarily reduces kinases CDK7, RPS6KA3, MET, and GAK. This compound (100 nM, 48 h) inhibits migration, invasion, and collagen deposition in A549 cells.

storage

Store at -20°C

References

[1]. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237.

GSK215 Preparation Products And Raw materials

Raw materials

Preparation Products

GSK215 Suppliers

Global( 34)Suppliers
Supplier Tel Email Country ProdList Advantage
Hubei Chuchang Biotech Co., Ltd.
+86-18727130788 +86-18727130788 info@chuchangbiotech.com China 109 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10522 58
Nantong HI-FUTURE Biology Co., Ltd. 		+undefined18051384581 sales@chemhifuture.com China 3136 58
LEAPCHEM CO., LTD. 		+86-852-30606658 market18@leapchem.com China 43348 58
Aladdin Scientific 		+1-+1(833)-552-7181 sales@aladdinsci.com United States 52927 58
Wuhan Jingkang en Biomedical Technology Co., Ltd 		+8613720134139 orders@jknbiochem.com China 4692 58
Changzhou Borl Biotechnology Co.,LTD 13606124132;13656121842 luyan0021@163.com China 217 58
Shanghai Lollane Biological Technology Co.,Ltd. 021-52996696，15000506266 15000506266 China 4197 55
ShangHai Angti Biotechnology Co., Ltd. 13764913901 info@angtibio.com China 4869 55
ShangHai Biochempartner Co.,Ltd 17754423994 17754423994 2853530910@QQ.com China 8012 62
Supplier Advantage
Hubei Chuchang Biotech Co., Ltd.
58
Zhejiang J&C Biological Technology Co.,Limited 		58
Nantong HI-FUTURE Biology Co., Ltd. 		58
LEAPCHEM CO., LTD. 		58
Aladdin Scientific 		58
Wuhan Jingkang en Biomedical Technology Co., Ltd 		58
Changzhou Borl Biotechnology Co.,LTD 58
Shanghai Lollane Biological Technology Co.,Ltd. 55
ShangHai Angti Biotechnology Co., Ltd. 55
ShangHai Biochempartner Co.,Ltd 62

View Lastest Price from GSK215 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
GSK215 pictures 2024-07-13 GSK215
2743427-26-9
 US $0.00-0.00 / mg 1mg 98% 100G Hubei Chuchang Biotech Co., Ltd.
  • GSK215 pictures
  • GSK215
    2743427-26-9
  • US $0.00-0.00 / mg
  • 98%
  • Hubei Chuchang Biotech Co., Ltd.

2743427-26-9(GSK215)Related Search:

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GSK215 (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide 2743427-26-9 C50H59F3N10O6S