Eph inhibitor 1 is a potent Eph inhibitor.
| Molecular Weight | 303.32 |
| Formula | C17H13N5O |
| CAS Number | 861249-77-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (Need ultrasonic) |
| Storage | 4°C, protect from light |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Ta Xiao et al. J Hematol Oncol. Targeting EphA2 in cancer
[5] Laura Devis-Jauregui et al. Autophagy. Autophagy in the physiological endometrium and cancer
| Related Ephrin Receptor Products |
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| EphA2 agonist 1
EphA2 agonist 1 is a potent EphA2 receptor agonist.EphA2 agonist 1 is highly active and selective for EphA2 overexpressing glioma cells and stimulates EphA2 phosphorylation. |
| LDN-211904 oxalate
LDN-211904 oxalate is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM.LDN-211904 oxalate showed good metabolic stability in mouse liver microsomes.LDN-211904 oxalate was shown to be effective in inhibiting STAT3-activated CSC stemness in combination with cetuximab. |
| KYL peptide
KYL peptide is an antagonistic peptide that selectively targets EphA4, and its binding to the ligand-binding domain of EphA4 effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. In addition, KYL peptide can promote nerve regeneration after injury and modulate immune response. |
| Ifabotuzumab
Ifabotuzumab is an IgG1κ antibody (KD=610 pM) targeting EphA3. Ifabotuzumab is able to cause apoptosis of tumor cells and activate antibody-dependent cell-mediated cytotoxicity (ADCC), which disrupts the tumor vascular system. In addition, Ifabotuzumab reduces idiopathic pulmonary fibrosis (IPF) CCR10+ cells and ameliorates pulmonary fibrosis. |
| Urolithin D
Urolithin D is competitive and reversible antagonist of EphA receptors. |
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