3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)-
3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)- Basic information
- Product Name:
- 3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)-
- Synonyms:
-
- 3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)-
- PPDA-001
- ICEC0942 (CT7001) Free base
- ICEC-0942
- CT7001)
- ICEC 0942 (ICEC0942
- Samuraciclib
- (3R,4R)-4-(((7-(benzylamino)-3-isopropylpyrazolo[1,5-a]pyrimidin-5-yl)amino)methyl)piperidin-3-ol
- CAS:
- 1805833-75-3
- MF:
- C22H30N6O
- MW:
- 394.51
- Mol File:
- 1805833-75-3.mol
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3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)- Chemical Properties
- Density
- 1.30±0.1 g/cm3(Predicted)
- pka
- 14.69±0.40(Predicted)
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3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)- Usage And Synthesis
Uses
Samuraciclib can be used to treat tuberous sclerosis complex using cyclin dependent kinase 7 (CDK7) inhibitors.
in vivo
Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors[1].
The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts[1].
| Animal Model: | Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells[1]. |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; daily; for 14 days |
| Result: | At day 14, tumor growth was inhibited by 60%. |
IC 50
CDK7/CycH/MAT1: 41 nM (IC50); CDK2/cycE1: 578 nM (IC50); CDK1: 1.8 μM (IC50); CDK4: 49 μM (IC50); CDK5: 9.4 μM (IC50); CDK6: 34 μM (IC50); CDK9: 1.2 μM (IC50)
3-Piperidinol, 4-[[[3-(1-methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]-, (3R,4R)-Supplier
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