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  1. Epigenetics Apoptosis
  2. Histone Methyltransferase DNA Methyltransferase Apoptosis
  3. CM-272

CM-272 是一種首創(chuàng)的,有效的,選擇性的,底物競爭性的且可逆的雙重 G9a/DNA 甲基轉(zhuǎn)移酶 (DNMTs) 抑制劑。CM-272 具有抗腫瘤活性。CM-272 抑制 G9aDNMT1,DNMT3ADNMT3BGLP,IC50 分別為 8 nM,382 nM,85 nM,1200 nM 和 2 nM。CM-272 抑制細(xì)胞增殖并促進(jìn)細(xì)胞凋亡,誘導(dǎo)干擾素刺激的基因和免疫原性細(xì)胞死亡。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

CM-272 Chemical Structure

CM-272 Chemical Structure

CAS No. : 1846570-31-7

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10 mM * 1 mL in DMSO ¥2001
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1 mg ¥823
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5 mg ¥1900
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10 mg ¥3325
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25 mg ¥4957
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death[1].

IC50 & Target[1]

G9a

8 nM (IC50)

EHMT1/GLP/KMT1D

2 nM (IC50)

DNMT1

382 nM (IC50)

DNMT3A

85 nM (IC50)

DNMT3B

1200 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF-10A EC50
0.2 μM
Compound: 2;CM-272
Antitumor activity against human spontaneously immortalized CDH-/- MCF10A cells assessed as cell numbers measured after 48 hrs
Antitumor activity against human spontaneously immortalized CDH-/- MCF10A cells assessed as cell numbers measured after 48 hrs
[PMID: 34878770]
MCF-10A EC50
0.5 μM
Compound: 2;CM-272
Antitumor activity against human spontaneously immortalized wild type MCF-10A cells assessed as cell numbers measured after 48 hrs
Antitumor activity against human spontaneously immortalized wild type MCF-10A cells assessed as cell numbers measured after 48 hrs
[PMID: 34878770]
MM1.S GI50
1041 nM
Compound: 5; CM-272
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay
[PMID: 33661013]
MV4-11 GI50
269 nM
Compound: 12; CM-272
Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay
Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay
[PMID: 29953809]
OCI-Ly10 GI50
455 nM
Compound: 12; CM-272
Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay
Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay
[PMID: 29953809]
OCI-Ly10 GI50
455 nM
Compound: 5
Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay
Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay
[PMID: 29890830]
OCI-Ly3 GI50
409 nM
Compound: 12; CM-272
Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay
Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay
[PMID: 29953809]
OCI-Ly3 GI50
409 nM
Compound: 5
Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay
Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay
[PMID: 29890830]
體外研究
(In Vitro)

CM-272 (100-1000 nM;12-72 小時(shí);CEMO-1、MV4-11 和 OCI-Ly10 細(xì)胞系) 處理以劑量和時(shí)間依賴性方式抑制細(xì)胞增殖[1]。
CM-272 (100-1000 nM;24 小時(shí);CEMO-1、MV4-11 和 OCI-Ly10 細(xì)胞系) 處理可阻斷細(xì)胞周期進(jìn)程[1]。
CM-272 (100-1000 nM;12-72 小時(shí);CEMO-1、MV4-11 和 OCI-Ly10 細(xì)胞系) 處理以劑量和時(shí)間依賴性方式誘導(dǎo) ALL、AML 和 DLBCL 細(xì)胞系細(xì)胞凋亡[1]。
CM-272 處理CEMO-1急性淋巴細(xì)胞白血病 (ALL) 細(xì)胞系、MV4-11急性髓性白血病 (AML) 細(xì)胞系和OCI-Ly10細(xì)胞系48小時(shí)后彌漫性大 B 細(xì)胞淋巴瘤 (DLBCL) 細(xì)胞系,GI50 值分別為 218 nM、269 nM 和 455 nM,并且與 H3K9me2 和 5mC 的整體水平下降相關(guān)[1]。
CM-272 的處理活性依賴于腫瘤細(xì)胞中 I 型干擾素反應(yīng)的早期激活,可能導(dǎo)致腫瘤細(xì)胞中細(xì)胞自主免疫原性死亡的誘導(dǎo)[1]。

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

Cell Proliferation Assay[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 12 hours, 24 hours, 48 hours and 72?hours
Result: Inhibited cell proliferation in a dose- and time-dependent manner.

Cell Cycle Analysis[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 24 hours
Result: Blocked cell cycle progression.

Apoptosis Analysis[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 12 hours, 24 hours, 48 hours and 72?hours
Result: Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.
體內(nèi)研究
(In Vivo)

CM-272 (2.5 mg/kg;靜脈注射;每天;持續(xù) 28 天;雌性 Rag2 / γc / 小鼠) 處理顯著延長了 CEMO- 1 細(xì)胞異種模型[1]。

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

Animal Model: Female BALB/Ca-Rag2?/?γc?/? mice (6–8-week-old) with CEMO-1 cells[1]
Dosage: 2.5 mg/kg
Administration: Intravenous injection; daily; for 28 days
Result: Induced a statistically significant increase in overall survival (OS) in mice.
分子量

478.63

Formula

C28H38N4O3

CAS 號
性狀

固體

顏色

Light brown to brown

運(yùn)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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 125 mg/mL (261.16 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 2.0893 mL 10.4465 mL 20.8930 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 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(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?jiān)?個(gè)月內(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(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,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

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

    Solubility: ≥ 2.08 mg/mL (4.35 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 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。
動(dòng)物溶解方案計(jì)算器
請輸入動(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

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請輸入您的動(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。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)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(shí)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(dòng)物實(shí)驗(yàn)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(jǐn)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(xiàn)

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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?jiān)?個(gè)月內(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 2.0893 mL 10.4465 mL 20.8930 mL 52.2324 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 mL 10.4465 mL
10 mM 0.2089 mL 1.0446 mL 2.0893 mL 5.2232 mL
15 mM 0.1393 mL 0.6964 mL 1.3929 mL 3.4822 mL
20 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6116 mL
25 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
30 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7411 mL
40 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
50 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0446 mL
60 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8705 mL
80 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
100 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5223 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:
CM-272
目錄號:
HY-101925
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