TG-101209

SKU: orb1223596

Description

A potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM; also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM); inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with IC50 of 200 nM, induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3; attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera; also potently inhibits BRD4 with Kd of 123 nM.Bone Cancer Preclinical.

Key Properties

• CAS Number: 936091-14-4
• MW: 509.6668
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₅N₇O₂S
• SMILES: O=S(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O
• Target: JAK
• Solubility: 10 mM in DMSO

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SAR-317461

Quick Database Links

Gene Symbol

JAK