製品番号: HY-111502

Y06036

Name: Y06036
Brand: MedChemExpress
SKU: HY-111502
Price: 42.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with K_d value of 82 nM. Antitumor activity.

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純度: 98.57%
CAS 番号: 1832671-96-1
分子式: C₁₆H₁₅BrN₂O₅S
分子量:427.27

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Y06036 構造式

CAS 番号: 1832671-96-1

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Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with K_d value of 82 nM^[1]. Antitumor activity^[1].

IC₅₀ & Target

^[1]

BRD4(1)

82 nM (Kd)

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>5 μM Compound: 6i	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
CWR22R	IC₅₀	1.5 μM Compound: 6i	Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
DU-145	IC₅₀	>6 μM Compound: 6i	Antiproliferative activity against AR-negative human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against AR-negative human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
HeLa	IC₅₀	>5 μM Compound: 6i	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
HFL1	IC₅₀	18.2 μM Compound: 6i	Cytotoxicity against human HFL1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Cytotoxicity against human HFL1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
Hs-578T	IC₅₀	1 μM Compound: 6i	Antiproliferative activity against human Hs-578T cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human Hs-578T cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
HT-29	IC₅₀	0.4 μM Compound: 6i	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay	[PMID: 29566488]
LNCaP	IC₅₀	1.06 μM Compound: 6i	Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
LNCaP C4-2B	IC₅₀	2.62 μM Compound: 6i	Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
MCF7	IC₅₀	1 μM Compound: 6i	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
MV4-11	IC₅₀	0.4 μM Compound: 6i	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay	[PMID: 29566488]
NCI-H1975	IC₅₀	2.5 μM Compound: 6i	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
PC-3	IC₅₀	>3 μM Compound: 6i	Antiproliferative activity against AR-negative human PC-3 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-negative human PC-3 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
U2OS	IC₅₀	>5 μM Compound: 6i	Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 29566488]
VCaP	IC₅₀	0.63 μM Compound: 6i	Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability incubated for 144 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability incubated for 144 hrs by cell-titer glo assay	[PMID: 29566488]

体外実験

Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC₅₀: 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels^[1].

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

Cell Viability Assay^[1]

Cell Line:

LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells
Concentration:

0.001-100 μM
Incubation Time:

96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP
Result:

Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC₅₀s of 1.06, 2.62, 1.50, 0.63 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

22Rv1 cells
Concentration:

1,2,4,8, and 16 μM
Incubation Time:

48 hours
Result:

Resulted in significant down-regulation of both AR-fl and AR variants levels

体内実験

Y06036 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06036 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior^[1].

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

Animal Model:

Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdc^scid for C4-2B) with C4-2B mouse xenograft model^[1]
Dosage:

50 mg/kg, 100 μL
Administration:

Intraperitoneal (i.p.) injection, 5 times per week, 25 days
Result:

Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 70%.

化学情報

CAS 番号 1832671-96-1
性状 Solid
分子量 427.27
分子式 C₁₆H₁₅BrN₂O₅S
Color Light yellow to yellow
SMILES

BrC1=CC(S(=O)(NC2=C(OC)C=C(ON=C3C)C3=C2)=O)=C(OC)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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ACS Nano

Nanopore Discrimination of Protein-Small-Molecule Drug Complexes at Near-Atomic Resolution. [Abstract]

2026 May 12;20(18):13624-13635. PMID: 42046448

溶剤 & 溶解度

体外:

DMSO : 130 mg/mL (304.26 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

2.3404 mL

11.7022 mL

23.4044 mL

5 mM

0.4681 mL

2.3404 mL

4.6809 mL

10 mM

0.2340 mL

1.1702 mL

2.3404 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.17 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Zhang M, et al. Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). J Med Chem. 2018 Apr 12;61(7):3037-3058. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3404 mL	11.7022 mL	23.4044 mL	58.5110 mL
	5 mM	0.4681 mL	2.3404 mL	4.6809 mL	11.7022 mL
	10 mM	0.2340 mL	1.1702 mL	2.3404 mL	5.8511 mL
	15 mM	0.1560 mL	0.7801 mL	1.5603 mL	3.9007 mL
	20 mM	0.1170 mL	0.5851 mL	1.1702 mL	2.9256 mL
	25 mM	0.0936 mL	0.4681 mL	0.9362 mL	2.3404 mL
	30 mM	0.0780 mL	0.3901 mL	0.7801 mL	1.9504 mL
	40 mM	0.0585 mL	0.2926 mL	0.5851 mL	1.4628 mL
	50 mM	0.0468 mL	0.2340 mL	0.4681 mL	1.1702 mL
	60 mM	0.0390 mL	0.1950 mL	0.3901 mL	0.9752 mL
	80 mM	0.0293 mL	0.1463 mL	0.2926 mL	0.7314 mL
	100 mM	0.0234 mL	0.1170 mL	0.2340 mL	0.5851 mL

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Keywords

Y06036

1 Cited Publications

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Y06036

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