TG-101348

SKU: orb1223595

Description

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F; also inhibits FLT3 (IC50=15 nM) and RET (IC50=48 nM) kinases, weakly inhibits JAK3 (IC50=168 nM), >35-fold selectivity over JAK1/3 and Tyk2; shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation; also potently inhibits BRD4 with Kd of 168 nM.Bone Cancer Phase 3 Clinical.

Key Properties

• CAS Number: 936091-26-8
• MW: 524.6782
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₆N₆O₃S
• SMILES: O=S(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O
• Target: JAK
• Solubility: DMSO: ≥ 42 mg/mL

Bioactivity

• In Vivo:
  Animal model: C57Bl/6 mice induced by the JAK2V617F mutation. Dosage: 60 mg/kg, 120 mg/kg. Administration: Oral gavage; twice daily; for 42 days. Result: Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.

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

Fedratinib | SAR 302503 | TG101348 | TG 101348

Quick Database Links

Gene Symbol

JAK