Cat. No.: HY-176225

BY13

Name: BY13
Brand: MedChemExpress
SKU: HY-176225
Price: 640.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

BY13 is a SRC-3 PROTAC degrader with a DC₅₀ of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model.
(Pink: SRC-3 ligand (HY-101447); Blue: Cereblon ligand (HY-41547); Black: linker (HY-176226)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.17%
CAS No.: 3117131-00-4
화학식: C₃₅H₃₅N₉O₄
분자량:645.71

보관:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

BY13 Chemical Structure

CAS No.: 3117131-00-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biological Activity

제품 설명

BY13 is a SRC-3 PROTAC degrader with a DC₅₀ of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model^[1]. (Pink: SRC-3 ligand (HY-101447); Blue: Cereblon ligand (HY-41547); Black: linker (HY-176226)).

IC₅₀ & Target

ERα	SRC-3 0.031 μM (DC₅₀)

All PROTACs Isoforms :

All Estrogen Receptor/ERR Isoforms :

All Src Isoforms :

In Vitro

BY13 (0.1-10 μM, 24 h) dose-dependently reduces SRC-3 and ERα protein level in MCF-7 cells with 71% and 85% degradation, respectively^[1].
BY13 (0.01-10 μM, 36 h) potently inhibits proliferation of wild-type, mutant-type and drug-resistant breast cancer cells (IC₅₀ of 0.003-0.35 μM for MCF-7, LCC2 and MCF-7^{D538G/Y537S/EGFR} cells), and dose-dependently degrades SRC-3 and ERα in mutant-type cells (particularly in MCF-7^Y537S cells at 0.1 μM)^[1].
BY13 (0.1-10 μM, 3-48 h) effectively reduces SRC-3 and ERα protein level, superior to Fulvestrant (HY-13636), and reaches the maximal degradation after 36 h while almost no longer increase with time in LCC2 cells ^[1].
BY13 (0.01-20 μM, 36 h) dramatically decreases the protein level of SRC-3 (0.1 μM only) and ERα (1 μM only) (DC₅₀ of 0.031 μM for SRC-3) with subtype selectivity favoring SRC-1 over SRC-2 in MCF-7 cells^[1].
BY13 (0.01-5 μM, 24 h) down-regulates the protein level of AR while this effect is weaker compared to ERα in MCF-7 cells, and moderately inhibits AR-overexpressing LNCaP cells (IC₅₀: 1.43 μM)^[1].
BY13 (1 μM, 36 h) significantly reduces SRC-3 protein level depending on a ubiquitin proteasome system (UPS) pathway in MCF-7 cells (similar phenomena observed in LCC2 cells)^[1].
BY13 (1 μM, 6 h, 40-76°C) can enter tumor cells and directly bind to SRC-3 with significantly enhancement of the SRC-3 protein thermal stability at high temperature in MCF-7 cells^[1].
BY13 (10 μM, 6 h) induces the spatial proximity of SRC-3 and CRBN, followed by promoting the formation of the SRC-3-BY13-CRBN ternary complex in MCF-7 cells^[1].
BY13 (0.01-10 μM, 36 h) significantly increases the mRNA expression of SRC-3 with the increasing concentrations and effectively reduces the mRNA level of ERα in LCC2 cells^[1].
BY13 (1-20 μM, 48 h) significantly induces breast cancer cells apoptosis with enhancement of both early and late apoptosis in MCF-7 and LCC2 cells.
BY13 (5-20 μM, 48 h) dose-dependently arrests LCC2 cells in the G1 phase, and thecell proportion is significantly higher than that in the S phase.
BY13 (0.01-100 μM) has sufficient metabolic stability and an acceptable safety profile with IC₅₀ of 2.73 and 1.1 μM for CYP3A4 and hERG channel.

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

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells, LCC2 cells
Concentration:

0.01, 0.1, 1, 5, 10 μM
Incubation Time:

24 h
Result:

Degraded both SRC-3 and ERα protein in MCF-7 cells at 1 μM with 71% and 85% degradation, respectively.
Dose-dependently reduced SRC-3 and ERα protein level in MCF-7 cells without a canonical “hook effect” as well as significantly degrades SRC-3 and ERα in LCC2 cells, superior to Fulvestrant (HY-13636).
Down-regulated the protein level of AR while this effect is weaker compared to ERα in MCF-7 cells

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells, LCC2 cells
Concentration:

1 μM
Incubation Time:

MCF-7 cells (3, 6, 9, 12, 24, 36 h), LCC2 cells (3, 6, 9, 12, 24, 36, 48 h)
Result:

Effectively reduced the SRC-3 protein level after 24h and reached the maximal degradation in MCF-7 cells at 36 h. Significantly reduced the protein level of SRC-3 after only 9 h of treatment, and reached the maximal degradation in LCC2 cells at 36 h with almost no longer increase of degradation.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells, LCC2 cells
Concentration:

1 μM after 1 μM of MG-132, Bortezomib, Chloroquine or (BY13-Neg, SI-2 and Pomalidomide) for 2 h
Incubation Time:

36 h
Result:

Significantly reduced SRC-3 protein level depending on a ubiquitin proteasome system (UPS) pathway, but this effect was reversed by two proteasome inhibitors (MG-132, Bortezomib and SI-2) not by BY13-Neg in MCF-7 cells (similar symptoms observed in LCC2 cells).

Apoptosis Analysis^[1]

Cell Line:

MCF-7 cells, LCC2 cells
Concentration:

1, 5, 10, 20 μM
Incubation Time:

48 h
Result:

Effectively induced cell apoptosis with enhancement of both early and late apoptosis in MCF-7 cells at increased concentrations (35% maximal early apoptosis rate).
Mainly induced the late apoptosis at 1 μM, but resulted in early apoptosis at 10 μM and induced a strong early apoptotic effect at 20 μM (＞ 30% early apoptosis rate) in LCC2 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	AUC_0-∞	T_max
Mice	2 mg/kg	i.v.	3.44 h	147.85 ng/mL	318.39 ng·h/mL	367.1 ng·h/mL	/
Mice	20 mg/kg	p.o.	4.49 h	25.44 ng/mL	47.07 ng·h/mL	58.39 ng·h/mL	0.33 h
Mice	4 mg/kg	i.p.	3.46 h	31.19 ng/mL	49.14 ng·h/mL	55.19 ng·h/mL	0.33 h

In Vivo

BY13 (3-10 μM/kg, i.p., once every two days for 23 ?days) has strong antiendocrine-resistant activity through targeting the SRC-3 and ERα degradation with a high safety property, and improves the poor prognosis of endocrine-resistant breast cancer in LCC2 xenograft mice model^[1].

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

Animal Model:

Female Balb/c nude mice (4 weeks old) were injected subcutaneously into the right lower axilla with LCC2 cells (5 × 10⁶ cells/mouse) to induce LCC2 xenograft mice model^[1].
Dosage:

3, 5 10 μM/kg, Tamoxifen (10 μM/kg) and Fulvestrant (5 μM/kg)
Administration:

i.p., once every two days for 23  days after tumors reached approximately 100 mm³, and then collected sample at 36 day¹.
Result:

Significantly inhibited tumor growth at 3 μM/kg, with superior effect of 54% tumor growth inhibition rate 54% at 5 μM/kg.
Almost completely degraded SRC-3 protein within the tumor tissues at 3 μM/kg, and the protein levels of both SRC-3 and ERα were further decreased at 5 μM/kg.
Had a wide therapeutic window, without effect weight gain of mice model up to 10 μM/kg.
Had a high safety property without observable histopathological changes in the organ tissues of mice model during the administration period at 3 and 5 μM/kg.
Improved the poor prognosis of endocrine-resistant breast cancer with reducement of ki67 level in tumor tissues at 3 and 5 μM/kg.

Related Protocols :

Chemical Information

CAS No. 3117131-00-4
Appearance Solid
분자량 645.71
화학식 C₃₅H₃₅N₉O₄
Color Light yellow to brown
SMILES

C/C(C1=NC=CC=C1)=N\NC2=NC(C=CC=C3)=C3N2C4CN(C4)C5CCN(CC5)C6=CC=CC7=C6C(N(C7=O)C8C(NC(CC8)=O)=O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도

In Vitro:

DMSO : 50 mg/mL (77.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5487 mL

7.7434 mL

15.4868 mL

5 mM

0.3097 mL

1.5487 mL

3.0974 mL

10 mM

0.1549 mL

0.7743 mL

1.5487 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (301 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Liang J, et al. Intercepting the Downstream of the Estrogen Receptor Signaling Pathway: Discovery of a Potent and Efficient SRC-3 PROTAC Degrader for Overcoming Endocrine Resistance Breast Cancer. J Med Chem. 2025 Jun 12; 68(11):11516-11542. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5487 mL	7.7434 mL	15.4868 mL	38.7171 mL
	5 mM	0.3097 mL	1.5487 mL	3.0974 mL	7.7434 mL
	10 mM	0.1549 mL	0.7743 mL	1.5487 mL	3.8717 mL
	15 mM	0.1032 mL	0.5162 mL	1.0325 mL	2.5811 mL
	20 mM	0.0774 mL	0.3872 mL	0.7743 mL	1.9359 mL
	25 mM	0.0619 mL	0.3097 mL	0.6195 mL	1.5487 mL
	30 mM	0.0516 mL	0.2581 mL	0.5162 mL	1.2906 mL
	40 mM	0.0387 mL	0.1936 mL	0.3872 mL	0.9679 mL
	50 mM	0.0310 mL	0.1549 mL	0.3097 mL	0.7743 mL
	60 mM	0.0258 mL	0.1291 mL	0.2581 mL	0.6453 mL

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BY13

All PROTACs Isoforms

All Estrogen Receptor/ERR Isoforms

All Src Isoforms