AZ12672857
Modify Date: 2025-08-26 19:52:18
AZ12672857 structure
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Common Name | AZ12672857 | ||
|---|---|---|---|---|
| CAS Number | 945396-55-4 | Molecular Weight | 486.57 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H30N8O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of AZ12672857AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1]. |
| Name | AZ12672857 |
|---|
| Description | AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1]. |
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| Related Catalog | |
| Target |
EP4:1.3 nM (IC50) Src |
| In Vitro | AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM[1]. |
| References |
| Molecular Formula | C26H30N8O2 |
|---|---|
| Molecular Weight | 486.57 |
| InChIKey | QLFGDTPACJHLRY-UHFFFAOYSA-N |
| SMILES | CN(c1ccnc(Nc2cc(N3CCOCC3)cc(N3CCOCC3)c2)n1)c1cccc2[nH]ncc12 |
| Hazard Codes | Xi |
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Name: AUC (0 to 24 hrs) in nude mouse at 100 mg/kg, po
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL1274261
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Name: Fraction unbound in nude mouse plasma at at 100 mg/kg, po
Source: ChEMBL
Target: Plasma
External Id: CHEMBL1274265
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Name: Inhibition of EphB4 by acoustic dispensing assay
Source: ChEMBL
Target: Ephrin type-B receptor 4
External Id: CHEMBL1274251
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Name: Inhibition of EphB4 autophosphorylation expressed in CHOK1 cells
Source: ChEMBL
Target: Ephrin type-B receptor 4
External Id: CHEMBL1274252
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Name: ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake fl...
Source: ChEMBL
Target: N/A
External Id: CHEMBL3301363
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Name: Inhibition of CYP3A4 in human liver microsomes at 10 uM by fluorometric assay
Source: ChEMBL
Target: Cytochrome P450 3A4
External Id: CHEMBL1274254
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Name: ASTRAZENECA: Solubility in pH7.4 buffer using solid starting material using the metho...
Source: ChEMBL
Target: N/A
External Id: CHEMBL3301364
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Name: Inhibition of SRC at 10 uM
Source: ChEMBL
Target: Proto-oncogene tyrosine-protein kinase Src
External Id: CHEMBL1274256
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Name: Inhibition of CYP3A4 in human liver microsomes at 10 uM preincubated with compound fo...
Source: ChEMBL
Target: Cytochrome P450 3A4
External Id: CHEMBL1763680
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Name: Inhibition of LCK at 10 uM
Source: ChEMBL
Target: Tyrosine-protein kinase Lck
External Id: CHEMBL1274257
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