| Identification | Back Directory | [Name]
TGR-1202 (sulfate) | [CAS]
1532533-75-7 | [Synonyms]
TGR-1202 (sulfate)
Umbralisib sulfate
FGHFSOLOVRUJND-NTISSMGPSA-N
RP-5264 sulfate|||TGR-1202 sulfate|||RP-5264 sulfate | [Molecular Formula]
C31H26F3N5O7S | [MDL Number]
MFCD28386167 | [MOL File]
1532533-75-7.mol | [Molecular Weight]
669.63 |
| Hazard Information | Back Directory | [Uses]
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach[1][2][3][4]. | [in vivo]
Umbralisib sulfate (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25 in a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line[4]. | [IC 50]
PI3Kδ: 6.2 (Kd); PI3Kγ: 1400 (Kd); PI3Kα: >10000 (Kd); PI3Kβ: >10000 (Kd) | [References]
[1] Maharaj K, et al. The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells. Blood Adv. 2020 Jul 14;4(13):3072-3084. DOI:10.1182/bloodadvances.2020001800
[2] Burris HA 3rd, et al. Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study. Lancet Oncol. 2018 Apr;19(4):486-496. DOI:10.1016/S1470-2045(18)30082-2
[3] Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.
[4] Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99. DOI:10.1182/blood-2016-08-731240 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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