2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. DDO-2728

DDO-2728 (化合物 19) 是一种选择性 AlkB homologue 5 (ALKBH5) 抑制剂，其 IC50 为 2.97 μM。DDO-2728 增加 N6 methyladenosine (m6A) 修饰的丰度，诱导细胞凋亡和细胞周期阻滞。DDO-2728 在 MV4−11 异种移植模型中抑制肿瘤生长且具有良好的安全性，显示出靶向 ALKBH5 在癌症研究中的潜力。

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DDO-2728 Chemical Structure

DDO-2728 Chemical Structure

CAS No. : 3029515-97-4

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1 mg ￥2300
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5 mg ￥5700
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10 mg ￥9200
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DDO-2728 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N6 methyladenosine (m6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research[1].

IC50 & Target

AlkB homologue 5 (ALKBH5) IC50: 2.97 μM[1]
体外研究
(In Vitro)

DDO-2728 (0-40 μM, 48 h) 在浓度梯度上提高 MOLM-13、HEK293 和 MV4-11 细胞的 m6A 甲基化水平[1]。
DDO-2728 (0.01-100 μM, 72 h) 可抑制 MOLM-13 和 MV4-11 细胞的增殖，IC50s 分别为 0.45 和 1.2 μM，且对 HEK293 和 HUVEC 的毒性相对较弱[1]。
DDO-2728 (20 μM, 48 h) 显著阻滞 MOLM-13 和 MV4-11 细胞的细胞周期于 G1/M 期[1]。
DDO-2728 (5, 10 μM, 48 h) 浓度依赖性地诱导 MV4−11 和 MOLM-13 细胞凋亡[1]。
DDO-2728 (20 μM, 24 h) 降低了 MOLM-13 和 MV4−11 细胞中 TACC3 mRNA 的半衰期[1]。
DDO-2728 (0-10 μM, 48 h) 在 mRNA 和蛋白水平上显著降低 MOLM-13 和 MV4-11 细胞中 TACC3 和 c-Myc 的丰度[1]。
1.19
大鼠和人血浆与肝脏微粒体代谢稳定性[1]

Species Plasma T1/2 (min) Microsome T1/2 (min) Microsome CL (μL/min/mg)
Human 624 430 3.2
Rat 251 13.8 100.4

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

DDO-2728 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MOLM-13, MV4-11, HEK293, HUVEC
Concentration: 0.01-100 μM
Incubation Time: 72 h
Result: Inhibited the proliferation of MOLM-13 and MV4−11 cells with IC50s of 0.45 and 1.2 μM respectively, didn't show visual cytotoxicity in HEK293 and HUVECs under 1 μM.

Apoptosis Analysis[1]

Cell Line: MOLM-13, MV4-11
Concentration: 0, 5, 10 μM
Incubation Time: 48 h
Result: Induced cell apoptosis of MV4−11 and MOLM-13 cells concentration-dependently, apoptosis rate for MV4−11 increased from 7.17% to 55.4%, apoptosis rate for MOLM-13 increased from 6.49% to 31.5%.

Cell Cycle Analysis[1]

Cell Line: MOLM-13, MV4-11
Concentration: 20 μM
Incubation Time: 48 h
Result: Arrested the cell cycle of MOLM-13 and MV4−11 cells at the G1/M phase as no G2/M phase cells exist.
体内研究
(In Vivo)

DDO-2728 (10-40 mg/kg, 腹腔注射, 每日一次, 14 d) 可有效抑制 MV4−11 异种移植裸鼠的肿瘤生长[1]。
1.19
DDO-2728在大鼠体内的药动学参数[1]

Parameter Rat (i.v., 2mg/kg) Rat (i.p., 10mg/kg)
T1/2 (min) 36.7 ± 3.2 148.3 ± 4.6
Cmax (ng/mL) 13388.3 ± 784.5 2337.5 ± 295.7
Tmax (min) 30
AUC0-∞ (min·μg/mL) 404.3 ± 58.6 349.1 ± 26.1
Vz_F_obs (mL/kg) 263.6 ± 17.5 6177.6 ± 650.2
Cl_F_obs (mL/min/kg) 5.0 ± 0.5 28.8 ± 2.2
MRT (min) 77.8 ± 15.5 168.2 ± 1.2
F (%) 17.3

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

Animal Model: MV4−11 xenograft nude mice [1]
Dosage: 10, 20, and 40 mg/kg
Administration: Intraperitoneal injection (i.p.) daily for 14 d
Result: Inhibited tumor growth significantly even at a concentration of 10 mg/kg. No significant change in the weight of the mice and the main organs during the treatment, the organ weight of test group mice was the same as vehicle group, no obvious injury damage was observed in the HE staining images of organ tissues.
分子量

578.45

Formula

C28H17F3N4O7
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (216.09 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7288 mL 8.6438 mL 17.2876 mL
5 mM 0.3458 mL 1.7288 mL 3.4575 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

DDO-2728 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7288 mL 8.6438 mL 17.2876 mL 43.2189 mL
5 mM 0.3458 mL 1.7288 mL 3.4575 mL 8.6438 mL
10 mM 0.1729 mL 0.8644 mL 1.7288 mL 4.3219 mL
15 mM 0.1153 mL 0.5763 mL 1.1525 mL 2.8813 mL
20 mM 0.0864 mL 0.4322 mL 0.8644 mL 2.1609 mL
25 mM 0.0692 mL 0.3458 mL 0.6915 mL 1.7288 mL
30 mM 0.0576 mL 0.2881 mL 0.5763 mL 1.4406 mL
40 mM 0.0432 mL 0.2161 mL 0.4322 mL 1.0805 mL
50 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8644 mL
60 mM 0.0288 mL 0.1441 mL 0.2881 mL 0.7203 mL
80 mM 0.0216 mL 0.1080 mL 0.2161 mL 0.5402 mL
100 mM 0.0173 mL 0.0864 mL 0.1729 mL 0.4322 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.

Keywords:

DDO-27283029515-97-4DDO2728DDO 2728Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246MV4?11MOLM-13HEK293HUVECSD ratsnude miceALKBH5 inhibitorm6Acell apoptosiscycle arrestcanceracute myeloid leukemiaInhibitorinhibitorinhibit

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