E7449
E7449
CAS: 1140964-99-3
Molecular Formula: C18H15N5O
E7449 - Names and Identifiers
E7449 - Physico-chemical Properties
| Molecular Formula | C18H15N5O |
| Molar Mass | 317.34 |
| Density | 1.53±0.1 g/cm3(Predicted) |
| Solubility | DMSO: < 6.96 mg/mL |
| pKa | 9.51±0.20(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | E7449 inhibits PARP enzyme activity and captures PARP1 onto damaged DNA, a mechanism that enhances cytotoxicity. In colorectal cancer cell lines, E7449 may prevent Wnt/β-catenin signaling by inhibiting TNKS. E7449 can stabilize the axin and TNKS proteins, thereby degrading beta-catenin, significantly altering the expression of Wnt target genes. E7449 inhibits TNKS1 and TNKS2 (I. E., PARP5a and PARP5b) with an IC50 in the range of 50-100 nmol/L. E7449 did not significantly inhibit PARP3 or PARPs 6-16, had no activity on PARP9 and PARP13, and had only minimal signaling effect on PARP4 activity. |
| In vivo study | E7449 can enhance the effect of tumor chemotherapy. In a BRCA-deficient xenograft, a single agent exerts anti-tumor activity. E7449 does not possess single-agent anti-tumor activity in other in vivo models. The anti-tumor activity of E7449 was enhanced by binding to MEK inhibitors. E7449 at 30 or 100 mg/kg was well tolerated with no significant weight loss or death. Treatment with E7449 at a concentration of 100 mg/kg resulted in significant PARP inhibition, which persisted for at least 12 hours, returning to basal levels within 24 hours. |
E7449 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.151 ml | 15.756 ml | 31.511 ml |
| 5 mM | 0.63 ml | 3.151 ml | 6.302 ml |
| 10 mM | 0.315 ml | 1.576 ml | 3.151 ml |
| 5 mM | 0.063 ml | 0.315 ml | 0.63 ml |
Last Update：2024-01-02 23:10:35
E7449 - Reference Information
| biological activity | E7449 is a PARP1/2 dual-effect small molecule compound inhibitor with biological oral activity that can pass through the blood-brain barrier, and can also inhibit PARP5a/5b (ie TNKS1/2). IC50 for PARP1 and PARP2 was 1 nM and 1.2 nM, respectively. |
| target | TargetValue PARP1 () 1 nM PARP2 1.2 nM |
| Target | Value |
| PARP1 () | 1 nM |
| PARP2 | 1.2 nM |
| In vitro study | E7449 inhibits PARP enzyme activity and captures PARP1 onto damaged DNA, which is a mechanism that can improve cytotoxicity. In colorectal cancer cell lines, E7449 may be used to block Wnt/β-catenin signaling by inhibiting TNKS. E7449 can stabilize axin and TNKS proteins, thus degrading beta-catenin and significantly changing the expression of Wnt target genes. E7449 inhibits the IC50 of TNKS1 and TNKS2 (I. e. PARP5a and PARP5b) in the range of 50-100 nmol/L. E7449 does not significantly inhibit PARP3 or PARPs 6-16, has no activity on PARP9 and PARP13, and has only minimal signal effect on PARP4 activity. |
| in vivo study | E7449 can enhance the effect of tumor chemotherapy. In xenograft tumors with BRCA deficiency, antitumor activity can be exerted with a single agent. E7449 does not possess mono-drug antitumor activity in other in vivo models. The anti-tumor activity of E7449 was enhanced by binding to MEK inhibitors. E7449 at 30 or 100 mg/kg was well tolerated with no significant weight loss or death. The E7449 treatment concentration of 100 mg/kg can lead to significant PARP inhibition, which can last for at least 12 hours and return to the basal level within 24 hours. |
Last Update：2024-04-09 22:09:11
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Product Name: 8-(Isoindolin-2-ylmethyl)-1,2-dihydro-3H-pyridazino[3,4,5-de]quinazolin-3-one Request for quotationCAS: 1140964-99-3
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Mobile: +86-18621343501
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Product Name: E7449; 2X-121 Visit Supplier Webpage Request for quotationCAS: 1140964-99-3
Tel: 609-228-6898
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Product Name: E7449 Visit Supplier Webpage Request for quotation
CAS: 1140964-99-3
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CAS: 1140964-99-3
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