AZ 3146
9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
CAS: 1124329-14-1
Molecular Formula: C24H32N6O3
AZ 3146 - Names and Identifiers
AZ 3146 - Physico-chemical Properties
| Molecular Formula | C24H32N6O3 |
| Molar Mass | 452.55 |
| Density | 1.279 |
| Boling Point | 621.0±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to at least 25 mg/ml) |
| Appearance | solid |
| Color | Off-white |
| pKa | 8.29±0.10(Predicted) |
| Storage Condition | Store at +4°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| In vitro study | AZ3146 also inhibits FAK, JNK1 JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequential recruitment of Mad1 and Mad2 to kinetochores. House, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1-C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. AZ3146 also inhibited FAK,JNK1,JNK2 and Kit. AZ3146 significantly inhibited the phosphorylation of Mps1 in cells. The mitotic specific phosphate forms of Aurora B and BubR1 are not affected by AZ3146. AZ3146 did not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with Nocodazole and 2 μm AZ3146 only transiently delayed mitosis and subsequently replicated their genome, indicating that AZ3146 was able to block SAC. AZ3146 also inhibits the established SAC signal, which is not blocked by nocodazole, and AZ3146 significantly accelerates the end of mitosis. In other undisturbed mitoses, AZ3146 reduced the time to complete mitosis from 90 minutes in the control group to 32 minutes. Strikingly, ~ 90% AZ3146 treated HeLa cells had abnormal mitosis,-50% of cells entering anaphase did not adjust their chromosomes, and-30% of cells completing mitosis did not undergo significant chromosome segregation. AZ3146 had a significant effect on the centromeric localization of Mad2, reducing its level to ~ 15%, but its effect on Mad1 was not significant, and its level remained at ~ 60%. Prior to entry into the mitotic phase, Mps1 is inhibited by AZ3146 and subsequent aggregation of Mad1 and Mad2 to the centromere is prevented. However, if Mps1 is inhibited by AZ3146 after entering the mitotic phase, Mad1-C-Mad2 of the core complex remains bound to the centromere, but O-Mad2 does not fully aggregate. |
AZ 3146 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.21 ml | 11.049 ml | 22.097 ml |
| 5 mM | 0.442 ml | 2.21 ml | 4.419 ml |
| 10 mM | 0.221 ml | 1.105 ml | 2.21 ml |
| 5 mM | 0.044 ml | 0.221 ml | 0.442 ml |
Last Update：2024-01-02 23:10:35
AZ 3146 - Reference Information
| biological activity | AZ 3146 is a selective Mps1 inhibitor with an IC50 of about 35 nM, which is helpful for recruiting CENP-E (kinesin-related dynein) and has a slightly weaker effect on FAK, JNK1, JNK2 and Kit. AZ 3146 is a selective Mps1 inhibitor with an IC50 of about 35 nM, which helps to aggregate CENP-E (kinin-related dynein) and has a slightly weaker effect on FAK, JNK1, JNK2 and Kit. |
| in vitro study | AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~ 90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~ 50% enter anaphase without aligning all of their chromosomes, and ~ 30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~ 15%, but its effect on Mad1 is less pronounced, with levels remaining at ~ 60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1-C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibited the phosphorylation of Mps1 in cells. The mitotic-specific phosphoric forms of Aurora B and BubR1 were not affected by AZ3146. AZ3146 did not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells were treated with Nocodazole and 2 μM AZ3146, only briefly delayed mitosis, and subsequently re-replicated their genomes, indicating that AZ3146 was able to block SAC. AZ3146 will also inhibit the established SAC signal, which is not blocked by the nocodazole, and AZ3146 will also significantly accelerate the end of mitosis. In other undisturbed mitoses, AZ3146 reduced the time to complete mitosis from 90 min to 32 min in the control group. Remarkably, ~ 90% AZ3146-treated HeLa cells undergo abnormal mitosis, ~ cells that 50% enter the later stage of division do not adjust their chromosomes, ~ cells that 30% complete mitosis do not undergo obvious chromosome separation. AZ3146 has a significant effect on the centromere localization of Mad2, reducing its level to ~ 15%, but its effect on Mad1 is not obvious, and its level remains at ~ 60%. Before entering the mitotic phase, Mps1 was inhibited by AZ3146, and then the aggregation of Mad1 and Mad2 to centromere was prevented. However, if Mps1 is inhibited by AZ3146 after entering the mitotic phase, Mad1-C-Mad2 the core complex still binds to the centromere, but the O-Mad2 cannot fully aggregate. |
| target | TargetValue Mps1 (Cell-free say) ~ 35 nM |
| Target | Value |
| Mps1 (Cell-free assay) | ~35 nM |
Last Update：2024-04-09 20:52:54
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Product Name: AZ3146 Visit Supplier Webpage Request for quotationCAS: 1124329-14-1
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
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Product Name: AZ3146 Visit Supplier Webpage Request for quotationCAS: 1124329-14-1
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
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Product Name: 9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one Visit Supplier Webpage Request for quotation
CAS: 1124329-14-1
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View History
AZ 3146
1-[3-amino-2-(4-chlorobenzoyl)-6-methylthieno[2,3-b]pyridin-5-yl]ethanone
0131011-(2-Fluoro-5-nitrophenyl)-2,5-dimethyl-1H-pyrrole
Ethyl 2-Aminopropanoate Hydrochloride
1-[2-(benzyloxy)-3-bromo-4,6-dimethoxyphenyl]ethanone
12679-86-6
3(2H)-Pyridazinone, 4-chloro-5-(cyclohexylamino)-2-(2-oxopropyl)-
RNA Polymerase III Inhibitor
22694-65-1
2173194-53-9
1-[3-amino-2-(4-chlorobenzoyl)-6-methylthieno[2,3-b]pyridin-5-yl]ethanone
0131011-(2-Fluoro-5-nitrophenyl)-2,5-dimethyl-1H-pyrrole
Ethyl 2-Aminopropanoate Hydrochloride
1-[2-(benzyloxy)-3-bromo-4,6-dimethoxyphenyl]ethanone
12679-86-6
3(2H)-Pyridazinone, 4-chloro-5-(cyclohexylamino)-2-(2-oxopropyl)-
RNA Polymerase III Inhibitor
22694-65-1
2173194-53-9