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Cat. No.: HY-178009

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EGFR-IN-175

EGFR-IN-175 is an orally active and selective EGFR^{L858R/T790M/C797S} inhibitor with an IC₅₀ of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.

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화학식: C₃₃H₃₈N₁₀O₄S₂
분자량:702.85

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

EGFR-IN-175 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

EGFR^WT

125.9 nM (IC₅₀)

EGFR^LR/TM

76.88 nM (IC₅₀)

EGFR^LR/TM/CS

18.94 nM (IC₅₀)

All EGFR Isoforms :

All Akt Isoforms :

In Vitro

EGFR-IN-175 (Compound M49) inhibits proliferation of BaF3-EGFR^{L858R/T790M/C797S}, A431 and H1975 cells with IC₅₀ values of 0.77, 5.11 and 5.94 μM^[1].
EGFR-IN-175 (0.1-2.5 μM) dose-dependently downregulates phosphorylation levels of p-EGFR, p-AKT, and p-ERK in BaF3-TM cells^[1].
EGFR-IN-175 (0.1-2.5 μM, 48 h) induces apoptosis and G1 phase arrest in BaF3-TM cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:

BaF3-TM cells
Concentration:

0.1, 1 and 2.5 μM
Incubation Time:

48 h
Result:

Increased apoptosis rate, reaching 69.68% at 2.5 μM.
Upregulated protein expression of Cleaved-PARP and Cleaved-Caspase-3.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	CL	MRT_0-∞	T_1/2	T_max	F
Rat^[1]	1 mg/kg	i.v.	4661.67 ng/mL	8915.08 ng·h/mL	145.27 mL/h/kg	12.99 h	11.45 h	/	/
Rat^[1]	10 mg/kg	p.o.	230.07 ng/mL	7343.86 ng·h/mL	1328.26 mL/h/kg	25.56 h	6.1 h	24 h	12.14 %

In Vivo

EGFR-IN-175 (Compound M49) (30 mg/kg for i.p., 30-60 mg/kg for p.o., once a day for 14 days) inhibits tumor growth in BaF3-EGFR^{L858R/T790M/C797S} xenograft BALB/c nude mice^[1].

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

Animal Model:

BaF3-EGFR^{L858R/T790M/C797S} xenograft BALB/c nude mice models^[1]
Dosage:

30 mg/kg for i.p., 30 and 60 mg/kg for p.o
Administration:

Once a day for 14 days
Result:

Reduced tumor volume.
Reduced Ki67 and increased TUNEL-positive cells in tumors.
Downregulated p-EGFR.
Had no significant body weight loss and no toxicity to major organs.

Chemical Information

분자량 702.85
화학식 C₃₃H₃₈N₁₀O₄S₂
SMILES

O=C1C(C2=CC=CS2)=NC3=CN=C(NC4=CC=C(N5CCC(N6CCN(C)CC6)CC5)C=C4)N=C3N1C7=CN(S(=O)(C8CC8)=O)N=C7OC
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jiang W, et al. Direct Ser797 Interacted Pteridine-7(8H)-one Derivatives as Highly Selective and Orally Available EGFRL858R/T790M/C797S Inhibitors. J Med Chem. 2025 Sep 11;68(17):18463-18490. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

EGFR-IN-175

All EGFR Isoforms

All Akt Isoforms