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  2. Protein Tyrosine Kinase/RTK
  3. BMX Kinase
  4. CHMFL-BMX-078

CHMFL-BMX-078  (Synonyms: CHMFL-BMX 078)

目錄號(hào): HY-101267 純度: ≥98.0%
COA 產(chǎn)品使用指南 技術(shù)支持

CHMFL-BMX-078是高效的，選擇性的，不可逆的，類型II BMX激酶抑制劑，IC50值為11 nM。

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CHMFL-BMX-078 Chemical Structure

CHMFL-BMX-078 Chemical Structure

CAS No. : 1808288-51-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2753
In-stock
1 mg ￥800
In-stock
5 mg ￥2000
In-stock
10 mg ￥3200
In-stock
25 mg ￥5440
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.

IC50 & Target

IC50: 11 nM (BMX)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
5637 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 5637 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 5637 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
769-P GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 769-P cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 769-P cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
A498 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human A498 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human A498 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
ACHN GI50
4.93 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human ACHN cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human ACHN cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
BaF3 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
CHO GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
CWR22R GI50
3.45 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 22Rv1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 22Rv1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
DU-145 GI50
7.89 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human DU145 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human DU145 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
EJ GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human EJ cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human EJ cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
J82 GI50
5.78 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human J82 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human J82 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
PC-3 GI50
3.45 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human PC3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human PC3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
T-24 GI50
8.98 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human T24 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human T24 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
體外研究
(In Vitro)

Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC50=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding Kd of 81 nM, while for the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI50=0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC50=5.8 nM) than C496S mutant (EC50=459 nM) for the inhibition of BMX total tyrosine phosphorylation. CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

CHMFL-BMX-078 exhibits a short half-life (T1/2=0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable Cmax (13565.23 ng/mL) and AUC0-t (1386.41 ng/mL h) in iv injection. However, it is not absorbed by oral administration, indicating that this compound could be administrated through iv or ip injection when used as a research tool[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

625.67

Formula

C33H35N7O6
CAS 號(hào)
性狀

固體

顏色

Off-white to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 30 mg/mL (47.95 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.5983 mL 7.9914 mL 15.9829 mL
5 mM 0.3197 mL 1.5983 mL 3.1966 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.00 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.00 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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

純度: ≥98.0%

參考文獻(xiàn)
Kinase Assay
[1]

The kinase reaction system contains BMX or BTK, 1 μL of serially diluted CHMFL-BMX-078, and substrate Poly peptidewith 100 μM ATP. The reaction in each tube is started immediately by adding ATP and kept going for an hour under 37 °C. After the tube cooled for 5 min at room temperature, 5 μL solvent reactions are carried out in a 384-well plate. Then 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ATP within 40 min. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 30 min to produce a luminescence signal. Luminescence signal is measured with an automated plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: Six 8-week-old male Sprague?Dawley rats are fasted overnight before starting drug treatment via intravenous and oral administration. Animal blood collection time points are as follows. For groups 1, 3, and 5 (intravenous): 1 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h before and after administration is selected. For group 2, 4, and 6 (oral): 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h before and after dosing. The plasma is collected for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?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 1.5983 mL 7.9914 mL 15.9829 mL 39.9572 mL
5 mM 0.3197 mL 1.5983 mL 3.1966 mL 7.9914 mL
10 mM 0.1598 mL 0.7991 mL 1.5983 mL 3.9957 mL
15 mM 0.1066 mL 0.5328 mL 1.0655 mL 2.6638 mL
20 mM 0.0799 mL 0.3996 mL 0.7991 mL 1.9979 mL
25 mM 0.0639 mL 0.3197 mL 0.6393 mL 1.5983 mL
30 mM 0.0533 mL 0.2664 mL 0.5328 mL 1.3319 mL
40 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9989 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：
CHMFL-BMX-078
目錄號(hào)：
HY-101267
需求量：