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Gefitinib-based PROTAC 3 - ≥98%(HPLC), high purity , CAS No.2230821-27-7

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Gefitinib-based PROTAC 3 - ≥98%(HPLC), high purity , CAS No.2230821-27-7

Moligand™

≥98%(HPLC)

CAS#: 2230821-27-7
Formula: C₄₇H₅₇ClFN₇O₈S
Molecular Weight: 934.52
PubChem CID: 135156947

Item Number

G287801

Grouped product items
SKU	Size	Availability	Price
G287801-1mg	1mg	In stock	$31.90
G287801-5mg	5mg	In stock	$129.90
G287801-10mg	10mg	In stock	$216.90

Potent EGFR Degrader

Basic Description

Synonyms	Gefitinib-based Proteolysis-targeting Chimera 3;Iressa-based PROTAC 3;(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)be
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent EGFR Degrader. Comprises an EGFR inhibitorgefitinib(Iressa) conjugated to a VHL ligand via a linker. Induces EGFR degradation (DC50values are 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively). Exhibits no d
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Product Description	Product Introduction Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.

Associated Targets(Human)

NCI-H3255 (70 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EGFR Tclin VHL/EGFR (323 Activities)

Discover Target: EGFR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Names and Identifiers

IUPAC Name	(2S,4R)-1-[(2S)-2-[3-[2-[5-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypentoxy]ethoxy]propanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
INCHI	InChI=1S/C47H57ClFN7O8S/c1-29-42(65-28-53-29)31-11-9-30(10-12-31)25-50-45(59)38-22-33(57)26-56(38)46(60)43(47(2,3)4)55-41(58)15-18-63-20-19-62-16-7-6-8-17-64-40-23-34-37(24-39(40)61-5)51-27-52-44(34)54-32-13-14-36(49)35(48)21-32/h9-14,21,23-24,27-28,33,38,43,57H,6-8,15-20,22,25-26H2,1-5H3,(H,50,59)(H,55,58)(H,51,52,54)/t33-,38+,43-/m1/s1
InChi Key	NICKHWYZMNLEPJ-TZSMONEZSA-N
Canonical SMILES	CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O
Isomeric SMILES	CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O
PubChem CID	135156947
Molecular Weight	934.52

Database links

CAS Registry No.	2230821-27-7
PubChem CID	135156947

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3 results found

Lot Number	Certificate Type	Date	Item
J2129029	Certificate of Analysis	Aug 13, 2024	G287801
J2129030	Certificate of Analysis	Aug 13, 2024	G287801
J2129031	Certificate of Analysis	Aug 13, 2024	G287801

Chemical and Physical Properties

Solubility	Soluble in DMSO, the highest concentration (mg / ml): 100, the highest concentration (mm): 107.01; Soluble in ethanol, the highest concentration (mg / ml): 100, the highest concentration (mm): 107.01; Insoluble in water DMF: 25 mg / ml; DMF:PBS (pH 7.2)

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

References

1. Burslem GM, Smith BE, Lai AC, Jaime-Figueroa S, McQuaid DC, Bondeson DP, Toure M, Dong H, Qian Y, Wang J et al.. (2018) The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.. Cell Chem Biol, 25 (1): (67-77.e3). [PMID:29129716]

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