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MedKoo Cat#: 408187 | Name: GSK215
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK215 is a potent, selective, FAK-degrading Proteolysis Targeting Chimera (PROTAC) based on a binder for the VHL E3 ligase and the known FAK inhibitor VS-4718. In mice, a single dose of GSK215 induced rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels (≈96 h) and a marked PK/PD disconnect. This tool PROTAC molecule is expected to be useful for the study of FAK-degradation biology in vivo.

Chemical Structure

GSK215
GSK215
CAS#2743427-26-9

Theoretical Analysis

MedKoo Cat#: 408187

Name: GSK215

CAS#: 2743427-26-9

Chemical Formula: C50H59F3N10O6S

Exact Mass: 984.4292

Molecular Weight: 985.14

Elemental Analysis: C, 60.96; H, 6.04; F, 5.79; N, 14.22; O, 9.74; S, 3.25

Price and Availability

Size Price Availability Quantity
5mg USD 250.00 2 Weeks
10mg USD 450.00 2 Weeks
25mg USD 850.00 2 Weeks
50mg USD 1,450.00 2 Weeks
100mg USD 2,450.00 2 Weeks
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Related CAS #
No Data
Synonym
GSK215; GSK-215; GSK 215;
IUPAC/Chemical Name
(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
InChi Key
ZGSWGXNEXAXEGV-XFCHVEHOSA-N
InChi Code
InChI=1S/C50H59F3N10O6S/c1-29(31-12-14-32(15-13-31)44-30(2)56-28-70-44)57-47(67)40-23-34(64)26-63(40)48(68)45(49(3,4)5)60-43(65)27-61-18-20-62(21-19-61)33-16-17-38(41(22-33)69-7)59-42-24-39(36(25-55-42)50(51,52)53)58-37-11-9-8-10-35(37)46(66)54-6/h8-17,22,24-25,28-29,34,40,45,64H,18-21,23,26-27H2,1-7H3,(H,54,66)(H,57,67)(H,60,65)(H2,55,58,59)/t29-,34+,40-,45+/m0/s1
SMILES Code
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(NC4=NC=C(C(F)(F)F)C(NC5=CC=CC=C5C(NC)=O)=C4)C(OC)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 985.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Down K, Amour A, Anderson NA, Barton N, Campos S, Cannons EP, Clissold C, Convery MA, Coward JJ, Doyle K, Duempelfeld B, Edwards CD, Goldsmith MD, Krause J, Mallett DN, McGonagle GA, Patel VK, Rowedder J, Rowland P, Sharpe A, Sriskantharajah S, Thomas DA, Thomson DW, Uddin S, Hamblin JN, Hessel EM. Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode. J Med Chem. 2021 Sep 23;64(18):13780-13792. doi: 10.1021/acs.jmedchem.1c01102. Epub 2021 Sep 11. PMID: 34510892. 2: Law RP, Nunes J, Chung CW, Bantscheff M, Buda K, Dai H, Evans JP, Flinders A, Klimaszewska D, Lewis AJ, Muelbaier M, Scott-Stevens P, Stacey P, Tame CJ, Watt GF, Zinn N, Queisser MA, Harling JD, Benowitz AB. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs. Angew Chem Int Ed Engl. 2021 Oct 18;60(43):23327-23334. doi: 10.1002/anie.202109237. Epub 2021 Sep 17. PMID: 34416073.