733767-34-5
733767-34-5 structure
- Name: NSC 23766
- Chemical Name: NSC 23766,N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediaminetrihydrochloride
- CAS Number: 733767-34-5
- Molecular Formula: C24H35N7
- Molecular Weight: 421.58
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2016-09-24 04:36:53
- Modify Date: 2024-02-04 11:47:14
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NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase, used for cancer treatment.
| Name | NSC 23766,N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediaminetrihydrochloride |
|---|---|
| Synonyms |
N-(2-{[5-(Diethylamino)-2-pentanyl]amino}-6-methyl-4-pyrimidinyl)-2-methyl-4,6-quinolinediamine trihydrochloride
N-(2-{[5-(Diethylamino)pentan-2-yl]amino}-6-methylpyrimidin-4-yl)-2-methylquinoline-4,6-diamine trihydrochloride 4,6-Quinolinediamine, N-[2-[[4-(diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-, hydrochloride (1:3) NSC 23766 |
| Description | NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase, used for cancer treatment. |
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| Related Catalog | |
| In Vitro | NSC 23766 (100 μM) treatment effectively inhibits polar body emission in a dose-dependent manner. NSC 23766 (200 μM) increases the percentage of morphologically abnormal spindles of oocytes. In NSC 23766-treated oocytes, the p-MAPK protein expression is significantly decreased[2]. NSC23766 (50 μM) plus 100 ng/mL Jagged1, GDF9 and BMP15, reduces the number of germLine cell cysts and increases the number of primordial follicles[3]. NSC23766 significantly inhibits GTP-Rac1 activity and phosphorylation of Rac1-PAK, ERKs and p38 MAPK in the spinal dorsal horn neurons[4]. |
| In Vivo | NSC23766 (2.5 mg/kg/day, i.p.) significantly attenuates the onset of spontaneous diabetes in NOD mice, without significant effects on the growth (body weights) of the mice. NSC23766 significantly increases the expression of Rac1 and CHOP, a marker for ER-stress, in islets from NOD mice[1]. |
| Kinase Assay | Briefly, fresh spinal cord tissue of the lumbar enlargement is homogenised in the presence of protease and phosphatase inhibitors and lysed with buffer. After being centrifuged at 12,000× g for 5 min at 4°C, the supernatants are collected and incubated with PAK-PBD beads at 4°C on a rotator for 1 h and then the beads are pelleted through centrifugation at 5000× g for 3 min at 4°C. The resulting pellet is resuspended in LaemmLi buffer and boiled for 2 min. The bead samples are subjected to Western blot analysis. Total Rac1 in each sample is also determined by Western blot analysis. |
| Animal Admin | Balb/c control and NOD mice are at 7 weeks of age and are divided into four groups (n=8/group). At 8 weeks of age two groups of experimental animals (Balb/c and NOD) receive NSC23766 (2.5 mg/kg/day, i.p./daily) and other two groups, which serve as control Balb/c and NOD mice and receive equal volume of saline. The body weights and blood glucose are monitored every week for 34 weeks. |
| References |
| Density | 1.16g/cm3 |
|---|---|
| Boiling Point | 632.4ºC at 760 mmHg |
| Molecular Formula | C24H35N7 |
| Molecular Weight | 421.58 |
| Flash Point | 336.2ºC |
| PSA | 91.99000 |
| LogP | 8.02300 |
| Index of Refraction | 1.646 |
| Storage condition | 2-8℃ |