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XMD8-92 Sale

(Synonyms: 2-[[2-乙氧基-4-(4-羟基-1-哌啶基)苯基]氨基]-5,11-二氢-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮) 目录号 : GC11076

A selective ERK5 inhibitor

XMD8-92 Chemical Structure

Cas No.:1234480-50-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥777.00
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10mg
¥525.00
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50mg
¥2,048.00
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100mg
¥3,339.00
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500mg
¥14,175.00
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1g
¥25,515.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Human pancreatic cancer AsPC-1 cell line

Preparation method

The solubility of this compound in DMSO is >23.8 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 and 15 μM for 48 h

Applications

Significant dose-dependent downregulation of DCLK1 mRNA and protein were observed following treatment with 10 and 15 μM of XMD8-92. Furthermore, a nearly 60% reduction in c-MYC, KRAS and NOTCH1 mRNA in AsPC-1 cells treated with XMD8-92 was also found. These data demonstrated that treatment AsPC-1 cells with XMD8-92 led to downregulation of DCLK1, c-MYC, KRAS and NOTCH1 mRNA.

Animal experiment [1]:

Animal models

HeLa, A549 and LL/2 xenograft mouse model

Dosage form

50 mg/kg twice a day

Application

It was found that vehicle-treated tumors grew exponentially throughout the experiment, whereas treatment with XMD8-92 not only arrested the tumor growth but resulted in decrease in the tumor volume. Moreover, treatment with XMD8-92 resulted in a significant (>80%) reduction in tumor volume compared to control tumors. In addition, more than 2-fold decrease in the tumor weight following treatment with XMD8-92 was observed.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Sureban SM et al. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. Cancer Lett. 2014 Aug 28;351(1):151-61.

产品描述

IC50: XMD8-92 has been synthesized as a potent inhibitor of Mitogen-activated protein kinase 7 (MAPK7/BMK1; Kd = 80 nM). XMD8-92 blocks EGF-induced activation of BMK1 with IC50 of 240 nM [1].
The mitogen-activated protein kinases (MAPKs) are crucial components of signaling cascades that regulate numerous physiological processes. Four MAPK pathways have been identified thus far, including extracelluar-signal-regulated kinase 1/2 (ERK1/2), c-Jun-amino-terminal kinase (JNK), p38, and BMK1. XMD8-92 is a MAPKs kinase inhibitor with anti-cancer activity against lung and cervical cancers.
In vitro: In a previous study, XMD8-92 was shown to inhibit AsPC-1 cancer cell proliferation and tumor xenograft growth. In XMD8-92 treated tumors, significant downregulation of DCLK1was found and several of its downstream targets, including c-MYC, KRAS, NOTCH1, ZEB1, ZEB2, SNAIL, SLUG, OCT4, SOX2, NANOG, KLF4, LIN28, VEGFR1, and VEGFR2) via upregulation of tumor suppressor miRNAs, such as let-7a, miR-144, miR-200a-c, and miR-143/145. XMD8-92 was, however, not found to affect BMK1 downstream genes p21 and p53. These findings suggested that XMD8-92 treatment led to the inhibition of DCLK1 and downstream oncogenic pathways, which would be a promising chemotherapeutic agent against PDAC [2].
In vivo: In both immunocompetent and immunodeficient mice, XMD8-92 treatment was found to able to block the growth of lung and cervical xenograft tumors, respectively, by 95%. This remarkable anti-tumor effect of XMD8-92 in lung and cervical xenograft tumor models was due to its capacity to inhibit tumor cell proliferation through the PML suppressioninducted p21 checkpoint protein, as well as by blocking of the contribution of BMK1 in tumorassociated angiogenesis [3].
Clinical trial: XMD8-92 is still at preclinical development stage up to this point.
Reference:
[1] Yang Q, Lee JD. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011;17(11):3527-32.
[2] Sureban SM, May R, Weygant N, Qu D, Chandrakesan P, Bannerman-Menson E, Ali N, Pantazis P, Westphalen CB, Wang TC, Houchen CW. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. Cancer Lett. 2014;351(1):151-61.
[3] Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, et al. Pharmacological inhibition of
BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010;18:258–67.

Chemical Properties

Cas No. 1234480-50-2 SDF
别名 2-[[2-乙氧基-4-(4-羟基-1-哌啶基)苯基]氨基]-5,11-二氢-5,11-二甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮
化学名 2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one
Canonical SMILES CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C
分子式 C26H30N6O3 分子量 474.57
溶解度 ≥ 23.75 mg/mL in DMSO 储存条件 Store at 4°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mM 2.1072 mL 10.5359 mL 21.0717 mL
5 mM 0.4214 mL 2.1072 mL 4.2143 mL
10 mM 0.2107 mL 1.0536 mL 2.1072 mL
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