ChemicalBook > CAS DataBase List > GSK215

GSK215

Product Name: GSK215
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
Formula Weight: 985.14
MOL File: 2743427-26-9.mol

Less

GSK215 Property

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

Less

Hazard and Precautionary Statements (GHS)

Less

GSK215 Chemical Properties,Usage,Production

Uses

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. 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].

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.

in vivo

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C_max and t_max values of 526 ng/mL and 0.33 hours, respectively^[1].

Animal Model:	Male CD1 mice (P878/881A), 7-9 weeks^[1]
Dosage:	8 mg/kg
Administration:	Single subcutaneous injection
Result:	Caused a rapid and profound degradation of FAK in liver over time, with a maximal degradation of ~85% being achieved within 18 h. Endogenous FAK was found to still be reduced by ~60% at 96 h post-dose.The C_max and t_max were 526 ng/mL and 0.33 hours, respectively.

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

Less

GSK215 Suppliers

China 49 United States 2 Global 51

Changzhou Borl Biotechnology Co.,LTD

Tel: 13606124132;13656121842
Email: luyan0021@163.com
Country: China
ProdList: 235
Advantage: 58

Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.

Tel: 15387063101
Email: 2881924050@qq.com
Country: China
ProdList: 9960
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4757
Advantage: 55

ShangHai Angti Biotechnology Co., Ltd.

Tel: 13764913901
Fax: -
Email: info@angtibio.com
Country: China
ProdList: 4985
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 021-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2989
Advantage: 58

Shanghai Yu Ben Biotechnology Co., Ltd.

Tel: 021-61350663 15502154572
Fax: -
Email: 1639466865@qq.com
Country: China
ProdList: 494
Advantage: 58

Jilin Province Woda Biotechnology Co., Ltd.

Tel: 13504435624
Email: 1927928688@qq.com
Country: China
ProdList: 1615
Advantage: 58

Zhejiang J&C Biological Technology Co.,Limited

Tel: +1-2135480471
Email: sales@sarms4muscle.com
Country: China
ProdList: 10473
Advantage: 58

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: +86-0519-85788828 +86-13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3934
Advantage: 58

Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd

Tel: 15317229551
Fax: QQ:3607245178
Email: 15151849396@163.com
Country: China
ProdList: 989
Advantage: 58

ShangHai ChuanQian Chemcial Technique Centre

Tel: 15869524721
Email: 3525679403@qq.com
Country: China
ProdList: 4989
Advantage: 58

Chunchuang (Wuhan) Technology Co., Ltd

Tel: 15727060112
Email: yutianchun2007@126.com
Country: China
ProdList: 9814
Advantage: 58

Wuhan Topule

Tel: +86-02787215551 +86-19945035818
Fax: 027-87215551
Email: 2936752263@qq.com
Country: China
ProdList: 7986
Advantage: 58

Zhengzhou convergence chemical co., LTD

Tel: 0371-0371-55153829 18003835034
Email: 2853979819@qq.com
Country: China
ProdList: 9998
Advantage: 58

Nantong Hi-Future Biotechnology Co., Ltd

Tel: 18051384581
Email: sales@chemhifuture.com
Country: China
ProdList: 2998
Advantage: 58

Hubei Kele Fine Chemical Co., Ltd

Tel: 027-59101668 19945030958
Fax: 027-59101668
Email: 2881924765@qq.com
Country: China
ProdList: 7938
Advantage: 58

Wuhan Augda Biotechnology Co., Ltd

Tel: 15071299552
Fax: QQ:262933239
Email: 262933239@qq.com
Country: China
ProdList: 7048
Advantage: 58

Bide Pharmatech Ltd.

Tel: 400-1647117 13681763483
Email: product02@bidepharm.com
Country: China
ProdList: 59936
Advantage: 58

InvivoChem

Tel: 13549236410
Email: sales@invivochem.cn
Country: China
ProdList: 6753
Advantage: 58

TargetMol Chemicals Inc.

Tel: 4008200310
Email: marketing@tsbiochem.com
Country: China
ProdList: 24961
Advantage: 58

Hubei Lidu New Material Technology Co., Ltd.

Tel: 19307246857
Email: 2687203556@qq.com
Country: China
ProdList: 786
Advantage: 58

Xianning Shen Lan Biomedical Research and Development Co., Ltd.

Tel: 18171815831
Email: 1341138380@qq.com
Country: China
ProdList: 4310
Advantage: 58

Shanghai Tachizaki Biomedical Research Center

Tel: 18014399201
Email: sales@chemlab-tachizaki.com
Country: China
ProdList: 2742
Advantage: 58

Wuhan Jingkangen Biomedical Technology Co., Ltd

Tel: 13720134139 086-15871494362 13720134139
Email: orders@jknbiochem.com
Country: China
ProdList: 6614
Advantage: 58

Shanghai Easy CDMO Co.,Ltd

Tel: 021-61734564 13854185395;
Email: info@easycdmo.com
Country: China
ProdList: 10024
Advantage: 58

https://hanhongsci.com/

Tel: 021-54306202 18917919676
Email: info@hanhongsci.com
Country: China
ProdList: 29995
Advantage: 58

Shanghai?Medlife?Pharm-Tech?Co.,?Ltd

Tel: 021-59167510 18117107507
Email: vip@med-life.cn
Country: China
ProdList: 5002
Advantage: 58

Hubei Chuchang Chemical Co., Ltd

Tel: 18 15623560702
Email: info@chuchangbiotech.com
Country: China
ProdList: 162
Advantage: 58

Jilin Chinese Academy of Sciences-yanshen Technology

Tel: 18143011203
Email: ET-market@chemextension.com
Country: China
ProdList: 32034
Advantage: 58

Changsha Fuzhen Biotechnology Co.，LTD

Tel: 0731-13823398 15111215862
Email: 313359644@qq.com
Country: China
ProdList: 4161
Advantage: 58

RD International Technology Co., Limited

Tel: 18024082417
Email: market@ubiochem.com
Country: China
ProdList: 9835
Advantage: 58

Olix (Shanghai) Pharmaceutical Technology Co., Ltd

Tel: 17316404525 17316404525
Email: 209533805@qq.com
Country: China
ProdList: 9766
Advantage: 58

Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd

Tel: 025-58851090 17714375163
Email: 2881759498@qq.com
Country: China
ProdList: 13011
Advantage: 58

R&D Systems, Inc

Tel: 18003437475
Fax: 1-612-656-4400
Email: rdname@qq.com
Country: China
ProdList: 6960
Advantage: 58

Sangon Biotech (Shanghai) Co.,Ltd.

Tel: 400-821-026
Email: Sales@sangon.com
Country: China
ProdList: 6710
Advantage: 58

Cayman Chemical Company

Tel: 800-364-9897
Email: sales@caymanchem.com
Country: China
ProdList: 6838
Advantage: 58

Shanghai Shengxiu Biotechnology Co., Ltd.

Tel: 13761144602
Email: 3896578657@qq.com
Country: China
ProdList: 4483
Advantage: 58

Selleck Chemicals

Tel: 400-668-6834
Email: info@selleck.cn
Country: China
ProdList: 6071
Advantage: 58

Wuhan Jingkang en Biomedical Technology Co., Ltd

Tel: +8613720134139
Email: orders@jknbiochem.com
Country: China
ProdList: 5221
Advantage: 58

Hubei Chuchang Biotech Co., Ltd.

Tel: +undefined15623860702
Email: info@chuchangbiotech.com
Country: China
ProdList: 202
Advantage: 58

HANGZHOU LEAP CHEM CO., LTD.

Tel: +86-571-87711850
Email: market18@leapchem.com
Country: China
ProdList: 43339
Advantage: 58

Nantong HI-FUTURE Biology Co., Ltd.

Tel: +undefined18051384581
Email: sales@chemhifuture.com
Country: China
ProdList: 3135
Advantage: 58

Guangzhou Suyan Biotechnology Co., Ltd

Tel: 18818417021
Country: CHINA
ProdList: 127
Advantage: 58

Guangzhou Kegou Biotechnology Co., Ltd.

Tel: 18689410811
Country: CHINA
ProdList: 178
Advantage: 58

Guangzhou Squirrel Biotechnology Co., Ltd.

Tel: 17765276361
Country: CHINA
ProdList: 109
Advantage: 58

Neobioscience Co., Ltd.

Tel: --
Fax: --
Email: info@neobioscience.com
Country: CHINA
ProdList: 6207
Advantage: 58

Absin Bioscience Inc.

Tel: --
Fax: --
Email: chenjw@absin.cn
Country: CHINA
ProdList: 6208
Advantage: 58

Proteintech China

Tel: --
Fax: --
Email: Proteintech-CN@ptglab.com
Country: CHINA
ProdList: 6290
Advantage: 58

Less

View Lastest Price from GSK215 manufacturers

Hubei Chuchang Biotech Co., Ltd.

Product: GSK215 2743427-26-9
Price: US $0.00-0.00/mg
Min. Order: 1mg
Purity: 98%
Supply Ability: 100G
Release date: 2024-04-17

2743427-26-9, GSK215Related Search:

GSK 2033 2-((4-(benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl dihydrogen phosphate N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide GSK-2256098 GSK2837808A GSK6853 GSK-A1 S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide GSK864 GSK484 GSK J4 HCl GSK 2334470 GSK2982772 GSK2636771 Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]- GSK778 N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

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