PROTAC EGFR degrader 4

Name: PROTAC EGFR degrader 4
Brand: MedChemExpress
SKU: HY-146349
Rating: 4.5 (1 reviews)

Cat. No.: HY-146349 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR^del19 and EGFR^L858R/T790M degradation with DC₅₀s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC₅₀s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.

For research use only. We do not sell to patients.

PROTAC EGFR degrader 4 Chemical Structure

CAS No. : 2882845-50-1

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All EGFR Isoform Specific Products:

View All Isoforms

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	245 nM Compound: P3	Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
HCC827	IC₅₀	0.76 nM Compound: P3	Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
HepG2	IC₅₀	> 5000 nM Compound: P3	Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
NCI-H1975	IC₅₀	203 nM Compound: P3	Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]

In Vitro

PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFR^del19) and H1975 (EGFR^L858R/T790M) with IC₅₀s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively^[1].
PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFR^del19 degradation with a DC₅₀ values of 0.51 nM^[1].
PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines^[1].
PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

995.29

Formula

C₅₅H₇₀N₁₂O₄S

CAS No.

2882845-50-1

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCN4CCN(CC4)C5=CC=C(C=C5)NC6=NC=C7N=C(N(C7=N6)C8CCCC8)NC9=CC=CC=C9)=O)=O)O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (100.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0047 mL	5.0237 mL	10.0473 mL
5 mM	0.2009 mL	1.0047 mL	2.0095 mL
10 mM	0.1005 mL	0.5024 mL	1.0047 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.70%

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Data Sheet (271 KB) SDS (252 KB)

COA (247 KB) HNMR (305 KB) RP-HPLC (256 KB) LCMS (129 KB)

Handling Instructions (2659 KB)

References

[1]. Hong-Yi Zhao, Discovery of potent small molecule PROTACs targeting mutant EGFR. Eur J Med Chem. 2020 Dec 15;208:112781. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0047 mL	5.0237 mL	10.0473 mL	25.1183 mL
	5 mM	0.2009 mL	1.0047 mL	2.0095 mL	5.0237 mL
	10 mM	0.1005 mL	0.5024 mL	1.0047 mL	2.5118 mL
	15 mM	0.0670 mL	0.3349 mL	0.6698 mL	1.6746 mL
	20 mM	0.0502 mL	0.2512 mL	0.5024 mL	1.2559 mL
	25 mM	0.0402 mL	0.2009 mL	0.4019 mL	1.0047 mL
	30 mM	0.0335 mL	0.1675 mL	0.3349 mL	0.8373 mL
	40 mM	0.0251 mL	0.1256 mL	0.2512 mL	0.6280 mL
	50 mM	0.0201 mL	0.1005 mL	0.2009 mL	0.5024 mL
	60 mM	0.0167 mL	0.0837 mL	0.1675 mL	0.4186 mL
	80 mM	0.0126 mL	0.0628 mL	0.1256 mL	0.3140 mL
	100 mM	0.0100 mL	0.0502 mL	0.1005 mL	0.2512 mL