Umbralisib (hydrochloride)
CAT:
804-HY-12279C-03
Size:
10 mg
Price:
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- Availability: 24/48H Stock Items & 2 to 6 Weeks non Stock Items.
- Dry Ice Shipment: No
Umbralisib (hydrochloride)
- Product Name Alternative: TGR-1202 hydrochloride; RP5264 hydrochloride
- CAS Number: 1532533-78-0
- UNSPSC Description: Umbralisib (TGR-1202) hydrochloride 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 hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach[1][2][3][4].
- Target Antigen: Casein Kinase; PI3K
- Type: Reference compound
- Related Pathways: Cell Cycle/DNA Damage;PI3K/Akt/mTOR;Stem Cell/Wnt
- Field of Research: Cancer
- Assay Protocol: https://www.medchemexpress.com/TGR-1202-hydrochloride.html
- Purity: 99.04
- Solubility: DMSO : ≥ 150 mg/mL
- Smiles: O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=CC=C(F)C=C16.[H]Cl
- Molecular Weight: 608.01
- References & Citations: [1]Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.|[2]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|[3]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.|[4]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.
- Shipping Conditions: Room Temperature
- Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
- Clinical Information: Launched