PROTAC EGFR degrader 9

Name: PROTAC EGFR degrader 9
Brand: MedChemExpress
SKU: HY-161536
Rating: 4.5 (1 reviews)

Cat. No.: HY-161536 Purity: 98.35%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC₅₀ of 10.2 nM and a K_d of 240.2 nM against EGFR^{L858R/T790M/C797S}. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)).

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

PROTAC EGFR degrader 9 Chemical Structure

CAS No. : 2992670-33-2

Size	Stock	Quantity
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

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Cereblon

EGFR^{L858R/T790M/C797S}

10.2 nM (DC₅₀)

EGFR^{L858R/T790M/C797S}

240.2 nM (Kd)

EGFR^{del19 T790M C797S}

36.5 nM (DC₅₀)

EGFR^L858R/T790M

88.5 nM (DC₅₀)

EGFR^del19

75.4 nM (DC₅₀)

EGFR (WT)

>300 nM (DC₅₀)

In Vitro

The DC₅₀ of PROTAC EGFR degrader 9 (Compound C6) against EGFR^{Del19/T790M/C797S}, EGFR^L858R/T790M, EGFR^Del19, and EGFR^WT are 36.5, 88.5, 75.4, and >300 nM, respectively^[1].
PROTAC EGFR degrader 9 (1.2-300 nM; 24 h) degrades the EGFR^{L858R/T790M/C797S} protein in H1975-TM cells in a dose-dependent manner^[1].
PROTAC EGFR degrader 9 exhibits significant inhibitory effects on PC-9-TMb (harboring EGFR^{Del19/T790M/C797S}), H1975, PC-9, and A549 cells, with IC₅₀ values of 43.5 nM, 46.2 nM, 17.5 nM, and 97.5 nM, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:	H1975-TM cells
Concentration:	1.2 nM, 3.7 nM, 11nM, 33 nM, 100 nM, 300 nM
Incubation Time:	24 h
Result:	Degraded the EGFRL858R/T790M/C797S protein in H1975-TM cells.

Cell Cycle Analysis^[1]

Cell Line:	H1975-TM cells
Concentration:	5 nM, 10 nM, 20 nM
Incubation Time:	24 h
Result:	Arrested H1975-TM cells in the G0/G1 phase.

Apoptosis Analysis^[1]

Cell Line:	H1975-TM cells
Concentration:	33 nM, 100 nM, 300 nM
Incubation Time:	24 h
Result:	Promoted cell apoptosis.

In Vivo

PROTAC EGFR degrader 9 (Compound C6; 25-100 mg/kg; oral administration; once-daily; for 31 days) significantly reduces the level of EGFR protein in tumor tissues, inhibits EGFR phosphorylation, and blocks the activation of downstream signaling pathways^[1].

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

Animal Model:	BALB/c nude mice injected with H1975-TM^[1]
Dosage:	25 mg/kg, 100 mg/kg
Administration:	Oral administration; once-daily; for 31 days
Result:	Could effectively inhibit the NSCLC tumor growth in vivo without obvious toxicity.

Molecular Weight

899.98

Formula

C₄₅H₄₈F₃N₉O₆S

CAS No.

2992670-33-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C4=CN(C5=CC=CC=C54)S(=O)(CC)=O)=N3)C(F)(F)F)C=C2)CC1)NC6=CC=CC7=C6CN(C7=O)C8C(NC(CC8)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (111.11 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	1.1111 mL	5.5557 mL	11.1114 mL
5 mM	0.2222 mL	1.1111 mL	2.2223 mL
10 mM	0.1111 mL	0.5556 mL	1.1111 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.35%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (244 KB) HNMR (156 KB) RP-HPLC (254 KB) LCMS (233 KB)

Handling Instructions (2659 KB)

References

[1]. Yasheng Zhu, et al. Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation. J Med Chem. 2024 May 9;67(9):7283-7300. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1111 mL	5.5557 mL	11.1114 mL	27.7784 mL
	5 mM	0.2222 mL	1.1111 mL	2.2223 mL	5.5557 mL
	10 mM	0.1111 mL	0.5556 mL	1.1111 mL	2.7778 mL
	15 mM	0.0741 mL	0.3704 mL	0.7408 mL	1.8519 mL
	20 mM	0.0556 mL	0.2778 mL	0.5556 mL	1.3889 mL
	25 mM	0.0444 mL	0.2222 mL	0.4445 mL	1.1111 mL
	30 mM	0.0370 mL	0.1852 mL	0.3704 mL	0.9259 mL
	40 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6945 mL
	50 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5556 mL
	60 mM	0.0185 mL	0.0926 mL	0.1852 mL	0.4630 mL
	80 mM	0.0139 mL	0.0694 mL	0.1389 mL	0.3472 mL
	100 mM	0.0111 mL	0.0556 mL	0.1111 mL	0.2778 mL