Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C31H24F3N5O3 |
Molecular Weight | 571.5492 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC1=C(F)C=C(C=C1)C2=NN([C@@H](C)C3=C(C4=CC=CC(F)=C4)C(=O)C5=CC(F)=CC=C5O3)C6=C2C(N)=NC=N6
InChI
InChIKey=IUVCFHHAEHNCFT-INIZCTEOSA-N
InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1
Molecular Formula | C31H24F3N5O3 |
Molecular Weight | 571.5492 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Umbralisib (TGR-1202) is an orally available PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. The delta isoform of PI3K is strongly expressed in cells of hematopoietic origin and is believed to be important in the proliferation and survival of B-cell lymphocytes. Inhibition of PI3K delta signaling with umbralisib has demonstrated robust activity in numerous pre-clinical models and primary cells from patients with hematologic malignancies. Umbralisib is currently in Phase 3 clinical development in combination with Ublituximab for patients with hematologic malignancies.
Approval Year
Sample Use Guides
relapsed or refractory chronic lymphocytic leukaemia or mantle cell lymphoma: umbralisib orally once daily (400 mg, 600 mg, or 800 mg) and ibrutinib orally once daily (420 mg for chronic lymphocytic leukaemia or 560 mg for mantle cell lymphoma) until disease progression or unacceptable toxicity. Umbralisib plus ibrutinib is well tolerated and active in relapsed or refractory chronic lymphocytic leukaemia and mantle cell lymphoma, with a recommended phase 2 dose of umbralisib 800 mg once daily.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Oct 21 21:28:36 UTC 2019
by
admin
on
Mon Oct 21 21:28:36 UTC 2019
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Record UNII |
38073MQB2A
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
533016
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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NCI_THESAURUS |
C129825
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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FDA ORPHAN DRUG |
554216
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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NCI_THESAURUS |
C2152
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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FDA ORPHAN DRUG |
552216
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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Code System | Code | Type | Description | ||
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C104413
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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PRIMARY | |||
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1532533-67-7
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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PRIMARY | |||
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72950888
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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PRIMARY | |||
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TGR-1202 FREE BASE
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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PRIMARY | MedKoo CAT NO: 205938, CAS NO.: 1532533-67-7(free base), 1532533-75-7(sulfate)Description: TGR-1202, also known as RP5264 , is a highly specific, orally available, PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. Inhibition of PI3K delta signaling with TGR-1202 has demonstrated robust activity in numerous pre-clinical models and primary cells from patients with hematologic malignancies.(Last Updated: 9/24/2015) | ||
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10350
Created by
admin on Mon Oct 21 21:28:36 UTC 2019 , Edited by admin on Mon Oct 21 21:28:36 UTC 2019
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR |
IC50
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Drugs: Carfilzomib(Primary), TGR 1202(Primary)
Indication: Cancer
Focus: Adverse reactions, Therapeutic Use
Most Recent Event: 10 Dec 2015 New trial record
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