Shopping Cart
- Remove All
Your shopping cart is currently empty
GSK215
🥰Excellent
Catalog No. T67843Cas No. 2743427-26-9
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.
GSK215
🥰Excellent
Purity: 99.3%
Catalog No. T67843Cas No. 2743427-26-9
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $127 | In Stock | |
| 5 mg | $317 | In Stock | |
| 10 mg | $497 | In Stock | |
| 25 mg | $829 | In Stock | |
| 50 mg | $1,150 | In Stock | |
| 100 mg | $1,550 | In Stock |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "GSK215"
ARV-471
Cited
Vepdegestrant
T397102229711-68-4In house
Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.
- $265
Size
QTY
CitedDefactinib Cited
VS-6063, PF-04554878
T19961073154-85-4
Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.
- $31
Size
QTY
CitedPND-1186
VS-4718, SR-2516, PND1186, PND 1186
T19501061353-68-1
PND-1186 (VS-4718) is a specific and reversible FAK inhibitor with an IC50 of 1.5 nM.
- $30
Size
QTY
Masitinib
AB1010
T2609790299-79-5
Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.
- $31
Size
QTY
dBET6 Cited
T51301950634-92-0
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
- $48
Size
QTY
CitedY15 Cited
FAK Inhibitor 14, 1,2,4,5-Benzenetetramine tetrahydrochlor
T71194506-66-5
Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity, blocks tumor growth.
- $43
Size
QTY
CitedAU-15330
T399542380274-50-8In house
AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]
- $139
Size
QTY
Chloropyramine hydrochloride
Nilfan, Halopyramine hydrochloride, Alergosan
T02636170-42-9
Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.
- $33
Size
QTY
Ifebemtinib FA
BI-853520 FA（1227948-82-4 Free base)
T64167LIn house
Ifebemtinib FA (BI-853520 FA) is an orally active and potent inhibitor of adhesion patch kinase (FAK) with anticancer and antiproliferative activity for the study of ovarian and lung cancer.
- $163
Size
QTY
Roslin 2 bromide
Roslin-2, Roslin2, Benzylhexamethylenetetramine bromide
T2473029574-21-8In house
Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5, exhibiting anticancer effects.
- $44
Size
QTY
C004019
T678342417159-57-8In house
C004019 is a small molecule PROTAC capable of targeting tau for selective protein degradation from the cell, while recruiting tau and E3 ligase (Vhl) for selective enhancement of tau ubiquitination and proteollyzation. C004019 is a candidate for AD and related tau protein diseases.
- $263
Size
QTY
CCT367766
T149082229856-58-8In house
CCT367766 is a potent, PROTAC-based, third-generation, iso-functional pirin-targeted protein degradation probe (PDP) that depletes pirin expression at low concentrations.CCT367766 has an IC50 value of 490 nM for the CRBN-DDB1 complex.CCT367766 has a good affinity for recombinant pirin and CRBN. CCT367766 has a good affinity for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. cct367766 is a potent orally active protein that reduces the expression of pirin at low concentrations.
- $293
Size
QTY
Select Batch
Purity:99.3%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation. |
| In vitro | GSK215 induced degradation is proteasome and ubiquitin dependent. 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[1]. GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells. GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[1]. |
| In vivo | GSK215 (8 mg/kg; i.h.; once) degrades FAK, and exhibits the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1]. |
| Molecular Weight | 985.13 |
| Formula | C50H59F3N10O6S |
| Cas No. | 2743427-26-9 |
| Smiles | CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCN(CC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)CC2)ncc1C(F)(F)F |
| Relative Density. | 1.317 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 225.0 mg/mL (228.4 mM ), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy GSK215 | purchase GSK215 | GSK215 cost | order GSK215 | GSK215 chemical structure | GSK215 in vivo | GSK215 in vitro | GSK215 formula | GSK215 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.