SCH772984
SCH772984 Basic information
- Product Name:
- SCH772984
- Synonyms:
-
- SCH772984
- SCH772984/SCH-772984
- (3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide
- (R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide
- (3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide SCH772984
- (R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-
- SCH772984, >=98%
- (3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide, 98%, a selective inhibitor of ERK1/2
- CAS:
- 942183-80-4
- MF:
- C33H33N9O2
- MW:
- 587.67
- EINECS:
- 1592732-453-0
- Product Categories:
-
- Inhibitors
- api
- MAPK
- Mol File:
- 942183-80-4.mol
SCH772984 Chemical Properties
- Melting point:
- >214°C (dec.)
- Boiling point:
- 857.3±65.0 °C(Predicted)
- Density
- 1.353±0.06(20.0000℃)
- storage temp.
- Refrigerator
- solubility
- DMSO (Slightly)
- pka
- 12.05±0.40(Predicted)
- form
- Solid
- color
- Pale Yellow
- CAS DataBase Reference
- 942183-80-4
SCH772984 Usage And Synthesis
Description
The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens. SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively). It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 μM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS. It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.
Uses
SCH772984 is a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors and has nanomolar cellular potency in tumor cells with mutations in BRAF, NRA5, or KRAS and induces tumor regressions in xenograft models.
Definition
ChEBI: SCH772984 is a member of the class of indazoles that is 1H-indazole substituted by pyridin-4-yl and {[(3R)-1-(2-oxo-2-{4-[4-(pyrimidin-2-yl)phenyl]piperazin-1-yl}ethyl)pyrrolidin-3-yl]carbonyl}amino groups at positions 3 and 5, respectively. It is a potent inhibitor of mitogen-activated protein kinases ERK1 and ERK2 (IC50 = 4 and 1 nM, respectively) that exhibits anti-cancer properties. It has a role as an antineoplastic agent, an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an apoptosis inducer and an analgesic. It is a member of pyridines, a biaryl, a secondary carboxamide, a pyrrolidinecarboxamide, a member of indazoles, a tertiary amino compound, a N-acylpiperazine, a N-arylpiperazine, a member of pyrimidines, a N-alkylpyrrolidine and a tertiary carboxamide.
in vivo
SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression[1].
Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1].
| Animal Model: | Female nude mice bearing human LOX BRAFV600E tumors[1] |
| Dosage: | 12.5, 25, 50 mg/kg |
| Administration: | Intraperitoneal injection; twice daily for 14 days |
| Result: | Tumor regressions were observed at all doses, such as 17% at 12.5 mg/kg, 84% at 25 mg/kg, and 98% at 50 mg/kg). |
target
ERK1
IC 50
ERK2: 1 nM (IC50); ERK1: 4 nM (IC50)
SCH772984Supplier
- Tel
- 021-38015121 18438616290
- wulan@absin.cn
- Tel
- sales@boylechem.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 021-58950125
- info@chemexpress.com
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