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  2. Epigenetics
  3. Epigenetic Reader Domain
  4. Y06036

Y06036 是一種有效的選擇性 BET 抑制劑，可與 BRD4(1) 溴結(jié)構(gòu)域結(jié)合，Kd 值為 82 nM。具有抗腫瘤活性。

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Y06036 Chemical Structure

Y06036 Chemical Structure

CAS No. : 1832671-96-1

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規(guī)格 價格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
50 mg ￥2200
In-stock
100 mg ￥3600
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

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

IC50 & Target[1]

BRD4(1)

82 nM (Kd)

細胞效力
(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]
體外研究
(In Vitro)

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].

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
體內(nèi)研究
(In Vivo)

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].

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-Prkdcscid 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%.
分子量

427.27

Formula

C16H15BrN2O5S
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 130 mg/mL (304.26 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3404 mL 11.7022 mL 23.4044 mL
5 mM 0.4681 mL 2.3404 mL 4.6809 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.17 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.17 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 21.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.17 mg/mL (5.08 mM); 澄清溶液

    此方案可獲得 ≥ 2.17 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 21.7 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 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
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.

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產(chǎn)品名稱：
Y06036
目錄號：
HY-111502
需求量：