Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H19ClF3NO5.ClH |
| Molecular Weight | 506.299 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1CC[C@H]([C@@H]1CO)C2=C3OC(=CC(=O)C3=C(O)C=C2O)C4=CC=C(C=C4Cl)C(F)(F)F
InChI
InChIKey=QCWRANLELLMJSH-OJMBIDBESA-N
InChI=1S/C22H19ClF3NO5.ClH/c1-27-5-4-12(14(27)9-28)19-15(29)7-16(30)20-17(31)8-18(32-21(19)20)11-3-2-10(6-13(11)23)22(24,25)26;/h2-3,6-8,12,14,28-30H,4-5,9H2,1H3;1H/t12-,14+;/m1./s1
| Molecular Formula | C22H19ClF3NO5 |
| Molecular Weight | 469.838 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including
http://www.chemietek.com/voruciclib-details.aspx
http://www.pharmacodia.com/yaodu/html/v1/chemicals/95276ef6535840ec6e432a7fc28688cb.html
Curator's Comment: Description was created based on several sources, including
http://www.chemietek.com/voruciclib-details.aspx
http://www.pharmacodia.com/yaodu/html/v1/chemicals/95276ef6535840ec6e432a7fc28688cb.html
Voruciclib (also known as P1446A-05) is a flavone-based, potent and selective CDK 4/6 inhibitor with activity in multiple BRAF-mutant and wild type cell lines. It is currently in clinical trials in combination with BRAF inhibitor (PLX4032) to treat advanced BRAF-mutant melanoma. Voruciclib has significant inhibitory activity against cutaneous and uveal melanoma. Mechanistic studies revealed that P1446A-05 inhibits phosphorylation targets of CDK members, and induces cell cycle arrest and apoptosis irrespective of melanoma genotype or phenotype. Voruciclib Hydrochloride is in phase I clinical trials by Piramal Life Sciences for the treatment of chronic lymphocytic leukaemia and malignant melanoma.
Originator
Approval Year
Sample Use Guides
In Subjects With Advanced Refractory Malignancies:
Voruciclib available as 25mg,50mg,100mg capsule. Subjects will be enrolled at at different dose levels of P1446A-05 to be taken once a day for 14 days followed by 7 days rest.This constitutes one cycle of Voruciclib. Four such cycles will be administered.
Route of Administration:
Oral
Treatment of A375 (BRAFV600E/NRASWT), SK-MEL-63 (NRASQ61K/BRAFWT), and OCM-1 (uveal) revealed increases
in both sub-G1 fractionation and G2/M arrest at 5 uM Voruciclib; both changes were statistically significant compared to DMSO-treated controls. At lower Voruciclib concentrations (e.g. 0.5 uM), there appeared to be an increase in the G1 population.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:26:09 GMT 2023
by
admin
on
Sat Dec 16 08:26:09 GMT 2023
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| Record UNII |
8BEP29W01U
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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1000023-05-1
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8BEP29W01U
Created by
admin on Sat Dec 16 08:26:09 GMT 2023 , Edited by admin on Sat Dec 16 08:26:09 GMT 2023
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67409218
Created by
admin on Sat Dec 16 08:26:09 GMT 2023 , Edited by admin on Sat Dec 16 08:26:09 GMT 2023
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SALT/SOLVATE -> PARENT |
