XMD 8-92 trifluoroacetate
2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
CAS: 1234480-50-2
Molecular Formula: C26H30N6O3
XMD 8-92 trifluoroacetate - Names and Identifiers
XMD 8-92 trifluoroacetate - Physico-chemical Properties
| Molecular Formula | C26H30N6O3 |
| Molar Mass | 474.55 |
| Density | 1.301 |
| Boling Point | 741.8±70.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | 14.76±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | XMD8-92 is an ERK5/BMK1 inhibitor and also BRD4 inhibitor. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. XMD8-92 blocks cellular BMK1 activation and significantly suppresses tumor growth in lung and cervical tumor models and is well tolerated in animals. |
| Target | BRD4 |
| In vitro study | XMD8-92, by inhibiting the activation of BMK1, significantly induced p21 expression in cells, and mediated the inhibition of cancer cell proliferation. XMD8-92 the inhibitory effect of hydroxysafflor yellow A(HSYA) on hepatic stellate cell (HSC) activation was significantly abolished and HSYA-mediated down-regulation of MEF2C was blocked. XMD8-92, by inhibiting the activation of BMK1, significantly induced p21 expression in cells, and mediated the inhibition of cancer cell proliferation. XMD8-92 the inhibitory effect of hydroxysafflor yellow A(HSYA) on hepatic stellate cell (HSC) activation was significantly abolished and HSYA-mediated down-regulation of MEF2C was blocked. |
| In vivo study | XMD8-92 (50 mg/kg, I. P.) significantly inhibited the growth of xenografted human or syngeneic mouse tumors by blocking tumor cell proliferation and tumor-associated angiogenesis. XMD8-92 inhibits the growth of pancreatic tumor xenografts by significantly down-regulating DCLK1 and several of its downstream targets. XMD8-92 (50 mg/kg, I. P.) significantly inhibited the growth of xenografted human or syngeneic mouse tumors by blocking tumor cell proliferation and tumor-associated angiogenesis. XMD8-92 inhibits the growth of pancreatic tumor xenografts by significantly down-regulating DCLK1 and several of its downstream targets. |
XMD 8-92 trifluoroacetate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.107 ml | 10.536 ml | 21.072 ml |
| 5 mM | 0.421 ml | 2.107 ml | 4.214 ml |
| 10 mM | 0.211 ml | 1.054 ml | 2.107 ml |
| 5 mM | 0.042 ml | 0.211 ml | 0.421 ml |
Last Update：2024-01-02 23:10:35
XMD 8-92 trifluoroacetate - Reference Information
| biological activity | XMD8-92 is a potent selective BMK1/ERK5 inhibitor with a Kd of 80 nM. XMD8-92 is a potent and selective double inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET), with Kd values of 80 nM and 170 nM for ERK5 and BRD4(1) respectively. |
| in vitro study | XMD8-92 significantly induced p21 expression in cells by inhibiting BMK1 activation and mediated inhibition of cancer cell proliferation. XMD8-92 significantly abolished the inhibitory effect of hydroxysafflor yellow A(HSYA) on the activation of hepatic stellate cells (HSC) and blocked the down-regulation of MEF2C mediated by HSYA. XMD8-92, by inhibiting BMK1 activation, p21 expression in cells was significantly induced and mediated by inhibiting the proliferation of cancer cells. XMD8-92 significantly abolished the inhibitory effect of hydroxysafflor yellow A(HSYA) on the activation of hepatic stellate cells (HSC) and blocked the down-regulation of MEF2C mediated by HSYA. |
| in vivo study | XMD8-92 (50 mg/kg, intraperitoneal injection) significantly inhibited the growth of tumors in xenograft human or homologous mice by blocking tumor cell proliferation and tumor-related angiogenesis. XMD8-92 inhibit the growth of pancreatic tumor xenografts by significantly down-regulating DCLK1 and its downstream targets. XMD8-92 (50 mg/kg, intraperitoneal injection) significantly inhibited the growth of xenograft human or homologous mouse tumors by blocking tumor cell proliferation and tumor-related angiogenesis. XMD8-92 inhibit the growth of pancreatic tumor xenografts by significantly down-regulating DCLK1 and its downstream targets. |
| target | TargetValue BMK1 (Cell-Free Assay) 80 nM(Kd) BRD4 (1) (Cell-Free Assay) 170 nM(Kd) |
| Target | Value |
| BMK1 (Cell-free assay) | 80 nM(Kd) |
| BRD4 (1) (Cell-free assay) | 170 nM(Kd) |
Last Update：2024-04-10 22:29:15
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Product Name: 2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one Visit Supplier Webpage Request for quotationCAS: 1234480-50-2
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Product Name: 2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one Visit Supplier Webpage Request for quotationCAS: 1234480-50-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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