Product Name :
Umbralisib hydrochloride
Description:
Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM.
CAS:
1532533-78-0
Molecular Weight:
608.01
Formula:
C31H25ClF3N5O3
Chemical Name:
2-[(1S)-1-{4-amino-3-[3-fluoro-4-(propan-2-yloxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}ethyl]-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one hydrochloride
Smiles :
Cl.CC(C)OC1=CC=C(C=C1F)C1=NN([C@@H](C)C2OC3=CC=C(F)C=C3C(=O)C=2C2C=C(F)C=CC=2)C2=NC=NC(N)=C12
InChiKey:
QGVUVMVWYWMZIR-NTISSMGPSA-N
InChi :
InChI=1S/C31H24F3N5O3.ClH/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);1H/t16-;/m0./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM.|Product information|CAS Number: 1532533-78-0|Molecular Weight: 608.01|Formula: C31H25ClF3N5O3|Chemical Name: 2-[(1S)-1-{4-amino-3-[3-fluoro-4-(propan-2-yloxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}ethyl]-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one hydrochloride|Smiles: Cl.CC(C)OC1=CC=C(C=C1F)C1=NN([C@@H](C)C2OC3=CC=C(F)C=C3C(=O)C=2C2C=C(F)C=CC=2)C2=NC=NC(N)=C12|InChiKey: QGVUVMVWYWMZIR-NTISSMGPSA-N|InChi: InChI=1S/C31H24F3N5O3.ClH/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);1H/t16-;/m0.{{SET2} site|{SET2} Neuronal Signaling|{SET2} Biological Activity|{SET2} In Vivo|{SET2} custom synthesis|{SET2} Autophagy} /s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 150 mg/mL (246.71 mM). H2O : Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.{{Vemurafenib} web|{Vemurafenib} Autophagy|{Vemurafenib} Protocol|{Vemurafenib} Purity|{Vemurafenib} custom synthesis|{Vemurafenib} Autophagy} In human lymphoma and leukemia cell lines, Umbralisib (TGR-1202; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner.PMID:23773119 Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells.|In Vivo:|In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, Umbralisib (TGR-1202; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25.|Products are for research use only. Not for human use.|