DDC-01-163

Name: DDC-01-163
Brand: MedChemExpress
SKU: HY-139997
Rating: 4.5 (1 reviews)

Cat. No.: HY-139997 Purity: 99.05%: Data Sheet
COA

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DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer.
(Pink: EGFR ligand (HY-151048); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).

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

DDC-01-163 Chemical Structure

CAS No. : 2140806-84-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer^[1]. (Pink: EGFR ligand (HY-151048); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).

IC₅₀ & Target

EGFR^L858R/T790M

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	< 500 nM Compound: Example I-22	Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay	[PMID: 31413790]
BaF3	IC₅₀	28 nM Compound: Fig 1, Cpd 7	Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 35691176]
BaF3	IC₅₀	41 nM Compound: 5	Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation	[PMID: 35254067]
BaF3	IC₅₀	41 nM Compound: Fig 1, Cpd 7	Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 35691176]
BaF3	IC₅₀	50 nM Compound: Fig 1, Cpd 7	Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 35691176]
BaF3	IC₅₀	96 nM Compound: 14	Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth	[PMID: 35728507]
BaF3	IC₅₀	96 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation	[PMID: 35254067]
BaF3	IC₅₀	96 nM Compound: DDC-01-163	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs	[PMID: 36274273]

In Vitro

DDC-01-163 exhibits an IC₅₀ value of 45 nM against EGFR L858R/T790M^[1].
DDC-01-163 (72 h) shows an IC₅₀ value of 45 at 72 h against EGFR L858R/T790M, and exhibits an EC₅₀ of 0.096 μM against L858R/T790M mutant Ba/F3 cells, while the EC₅₀ against wild-type EGFR Ba/F3 cells was >10 μM^[1].
DDC-01-163 (5 h) bound CRBN more effectively than JBJ-07-038 in BRD4BD2 cells^[1].
DDC-01-163 (0.01-1 μM, 6-48 h) induces dose- and time-dependent EGFR degradation in Ba/F3 L858R/T790M cells, with maximum degradation occurring at 24 hours. A hook effect was observed at higher concentrations, while no degradation was observed in wild-type Ba/F3 cells^[1].
DDC-01-163 (0.1-1 μM, 0-72 h) induces time-dependent EGFR degradation in H1975 cells, with maximum degradation occurring between 24 and 48 hours^[1].
DDC-01-163 (0.1 μM, 72 h), when combined with Osimertinib, enhances the anti-proliferative activity and EGFR phosphorylation inhibition in L858R/T790M Ba/F3 cells, whereas high-dose Osimertinib (0.1 μM) exerted an antagonistic effect^[1].
DDC-01-163 (72 h) effectively inhibits the proliferation of Ba/F3 cells stably transfected with L858R/T790M/C797S (EC₅₀ = 0.041 μM) or L858R/T790M/L718Q EGFR (EC₅₀ = 0.028 μM) mutations^[1].

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

Western Blot Analysis^[1]

Cell Line:	L858R/T790M Ba/F3 cells
Concentration:	0.01 μM, 0.1 μM, 1 μM
Incubation Time:	6 h, 24 h, 48 h
Result:	In L858R/T790M mutant Ba/F3 cells, dose- and time-dependent EGFR degradation was induced, with maximum degradation (59-62%) occurring at 24 hours and persisting until 48 hours. A hook effect (degradation decreased) was observed at higher concentrations (1 μM).

Molecular Weight

942.05

Formula

C₄₉H₅₁N₉O₉S

CAS No.

2140806-84-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCN4CCN(CC4)C5=CC=C(C6=CC=C7C(C(N(C(C8=CC=CC=C8)C(NC9=NC=CS9)=O)C7)=O)=C6)C=N5)=CC=C3)=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 : 50 mg/mL (53.08 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	1.0615 mL	5.3076 mL	10.6151 mL
5 mM	0.2123 mL	1.0615 mL	2.1230 mL
10 mM	0.1062 mL	0.5308 mL	1.0615 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
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.05%

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Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) HNMR (391 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Jang J, et al. Mutant-Selective Allosteric EGFR Degraders Are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481–14489.

[2]. Jaebong Jang, et al. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489. [Content Brief]

[3]. Surya Kant Tripathi, et al. Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma. Drug Discov Today. 2021 Jun;26(6):1466-1472. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0615 mL	5.3076 mL	10.6151 mL	26.5379 mL
	5 mM	0.2123 mL	1.0615 mL	2.1230 mL	5.3076 mL
	10 mM	0.1062 mL	0.5308 mL	1.0615 mL	2.6538 mL
	15 mM	0.0708 mL	0.3538 mL	0.7077 mL	1.7692 mL
	20 mM	0.0531 mL	0.2654 mL	0.5308 mL	1.3269 mL
	25 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0615 mL
	30 mM	0.0354 mL	0.1769 mL	0.3538 mL	0.8846 mL
	40 mM	0.0265 mL	0.1327 mL	0.2654 mL	0.6634 mL
	50 mM	0.0212 mL	0.1062 mL	0.2123 mL	0.5308 mL

DDC-01-163 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DDC-01-1632140806-84-2PROTACsEGFREpidermal growth factor receptorErbB-1HER1CRBNBa/F3L858R/T790MAllostericPROTACDrug-Resistant MutationInhibitorinhibitorinhibit

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DDC-01-163

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