217366
PLX647
Size
£492.00
- SKU:
- 217366
- Molecular Weight:
- 382.4
- Storage Conditions:
- -20°C
- Supplier:
- United States Biological
- CAS Number:
- 873786-09-5
- Extra Details:
- PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively). It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain. Synonyms: 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine CAS No: 873786-09-5 Molecular Weight: 382.4 Molecular Formula: C₂₁H₁₇F₃N₄ Solubility: DMF, DMSO, DMSO:PBS(pH 7.2) (1:3) λmax: 224, 245, 293 nm Appearance: Crystalline solid Purity: ≥95% Storage and Stability: Store at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
- Shipping Conditions:
- Blue Ice