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SML3281

GSK215 hydrochloride

≥98% (HPLC)

Synonym(s):

GSK 215 hydrochloride, (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-(4-(2-(methylcarbamoyl)phenylamino)-5-(trifluoromethyl)pyridin-2-ylamino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide hydrochloride, GSK-215 hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C50H59F3N10O6S · xHCl
Molecular Weight:
985.13 (free base basis)
UNSPSC Code:
51111800
NACRES:
NA.21
MDL number:
MFCD34574613
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

composition

, 0-8 (H2O), , 1.8-3.3 mol (HCl)

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

FC(F)(F)c1cnc(cc1Nc7c(cccc7)C(=O)NC)Nc2c(cc(cc2)N3CCN(CC3)CC(=O)N[C@@H](C(C)(C)C)C(=O)N4[C@@H](C[C@H](C4)O)C(=O)N[C@@H](C)c5ccc(cc5)c6[s]cnc6C)OC

InChI key

ZGSWGXNEXAXEGV-XFCHVEHOSA-N

Biochem/physiol Actions

GSK215 is a potent and selective focal adhesion kinase (FAK) degrader (DC50 = 1.3 nM; A549 cells) composed of the FAK inhibitor VS-4718 and the VHL E3 ligase binder VHL-021. GSK215 shows cell type-dependent growth inhibition, where it inhibits A549 (IC50 <1 µM) and MCF-7 (IC50 <0.1 µM), but not BT474, in 2D cultures, while the growth of BT47 (IC50 <0.1 µM) and MCF-7 (IC50 ~0.1 µM), but not A5494, are inhibited by GSK215 in 3D cultures.
Potent and selective focal adhesion kinase (FAK) degrader composed of the FAK inhibitor VS-4718 and the VHL E3 ligase binder VHL-021.

Disclaimer

Hygroscopic

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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