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  2. Cell Cycle/DNA Damage Apoptosis
  3. Antifolate Apoptosis Caspase Bcl-2 Family
  4. Lometrexol

Lometrexol (DDATHF) 是一種抗嘌呤類抗葉酸 (antifolate) 藥，可抑制甘氨酰胺核糖核苷酸甲酰基轉(zhuǎn)移酶 (GARFT) 的活性，但不會引起可檢測水平的 DNA 鏈斷裂。Lometrexol 可以進一步抑制嘌呤從頭合成，導(dǎo)致異常的細(xì)胞增殖，凋亡 (apoptosis) 和細(xì)胞周期停滯。Lometrexol 具有抗癌活性。Lometrexol 還是一種有效的人絲氨酸羥甲基轉(zhuǎn)移酶 1/2 (hSHMT1/2) 抑制劑。

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Lometrexol Chemical Structure

Lometrexol Chemical Structure

CAS No. : 106400-81-1

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2145
In-stock
1 mg ￥860
In-stock
5 mg ￥1950
In-stock
10 mg ￥2850
In-stock
25 mg ￥4740
In-stock
50 mg 現(xiàn)貨 詢價
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
0.007 μg/mL
Compound: 1 (DDATHF)
The compound was tested for its cytotoxicity against CCRF-CEM human leukemic cells using 72 hrs assay
The compound was tested for its cytotoxicity against CCRF-CEM human leukemic cells using 72 hrs assay
10.1016/S0960-894X(01)80214-6
IGROV-1 IC50
16 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid
Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid
[PMID: 21879757]
IGROV-1 IC50
3.1 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs
Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs
[PMID: 21879757]
IGROV-1 IC50
5.77 nM
Compound: LMTX
Inhibition of GARFTase in human IGROV1 cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs in complete folate free RPMI medium in presence of 2 nM leucovorin
Inhibition of GARFTase in human IGROV1 cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs in complete folate free RPMI medium in presence of 2 nM leucovorin
[PMID: 22243528]
KB IC50
1.2 nM
Compound: LMTX, Lometrexol
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay
[PMID: 24111942]
KB IC50
1.2 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs
Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs
[PMID: 21879757]
KB IC50
14 nM
Compound: LMX
Inhibition of GARFTase in human KB cells assessed as inhibition of incorporation of [14C]glycine into [14C]formyl GAR after 30 mins in presence of azaserine
Inhibition of GARFTase in human KB cells assessed as inhibition of incorporation of [14C]glycine into [14C]formyl GAR after 30 mins in presence of azaserine
[PMID: 19371039]
KB IC50
14 μM
Compound: LMTX, (R)-6-DDATHF
Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay
Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay
[PMID: 20085328]
KB IC50
31 nM
Compound: LMTX, Lometrexol
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid
[PMID: 24111942]
KB IC50
31 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid
Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid
[PMID: 21879757]
R2 IC50
> 1000 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs
Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs
[PMID: 21879757]
R2 IC50
12 nM
Compound: LMTX; (6R)-5,10-dideazatetrahydrofolate
Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis
Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis
[PMID: 27458733]
R2 IC50
29.7 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days
[PMID: 21879757]
R2 IC50
38 nM
Compound: LMTX, Lometrexol
Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay
Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay
[PMID: 24111942]
R2 IC50
38 nM
Compound: LMTX, lometrexol
Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay
Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay
[PMID: 24256410]
R2 IC50
38 nM
Compound: LMTX, Lometrexol, 6-(R)DDATHF
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs
[PMID: 21879757]
體外研究
(In Vitro)

Lometrexol (DDATHF) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3].
Lometrexol (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells[3].
Lometrexol (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells[3].

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

Cell Viability Assay[3]

Cell Line: Mouse leukemia L1210 cells
Concentration: 1, 30 μM
Incubation Time: 2, 4, 6, 8, 10 hours
Result: Induced rapid and complete growth inhibition.

Cell Cycle Analysis[3]

Cell Line: L1210 cells
Concentration: 1 μM
Incubation Time: 2, 4, 8, 12, 24 hours
Result: Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase.
體內(nèi)研究
(In Vivo)

Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) induces neural tube defects (NTDs) by disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner[1].
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels[1].
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].

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

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 15, 30, 35, 40, 45 and 60 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
Result: Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.
Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 4 days
Result: Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
Clinical Trial
分子量

443.45

Formula

C21H25N5O6
CAS 號
性狀

固體

顏色

White to light yellow

中文名稱

洛美曲索
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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (225.50 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 2.2550 mL 11.2752 mL 22.5505 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 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，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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(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(dāng)保存；體內(nèi)實驗的工作液，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: ≥ 5 mg/mL (11.28 mM); 澄清溶液

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (11.28 mM); 澄清溶液

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： 0.5% CMC-Na/saline water

    Solubility: 25 mg/mL (56.38 mM); 懸濁液; 超聲助溶

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(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

純度: 98.96%

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(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，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.2550 mL 11.2752 mL 22.5505 mL 56.3761 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 mL 11.2752 mL
10 mM 0.2255 mL 1.1275 mL 2.2550 mL 5.6376 mL
15 mM 0.1503 mL 0.7517 mL 1.5034 mL 3.7584 mL
20 mM 0.1128 mL 0.5638 mL 1.1275 mL 2.8188 mL
25 mM 0.0902 mL 0.4510 mL 0.9020 mL 2.2550 mL
30 mM 0.0752 mL 0.3758 mL 0.7517 mL 1.8792 mL
40 mM 0.0564 mL 0.2819 mL 0.5638 mL 1.4094 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1275 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9396 mL
80 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7047 mL
100 mM 0.0226 mL 0.1128 mL 0.2255 mL 0.5638 mL
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    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：
Lometrexol
目錄號：
HY-14521
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