SB1317 hydrochloride (1204918-72-8(free base))

SKU: orb1303042

Description

SB1317 hydrochloride (1204918-72-8(free base))

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• MW: 408.92
• Purity: 99.84% (May vary between batches)
• Formula: C₂₃H₂₅ClN₄O
• SMILES: Cl.CN1C\C=C\CCOc2cccc(c2)-c2ccnc(Nc3cccc(C1)c3)n2
• Target: JAK,CDK,FLT
• Solubility: DMSO:60 mg/mL (146.73 mM)

Bioactivity

• Target IC50:
  CDK2:13nM|FLT3:56 nM|JAK2:73nM
• In Vivo:
  SB1317 (75 mg/kg/day, p.o., 3×/week) markedly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose (50 mg/kg/day, p.o., 3×/week) is marginally effective. Treatment with SB1317 using either regime significantly inhibits the growth of tumors with mean TGIs of 42% (p.o.) and 63% (i.p.), respectively. In pharmacokinetic studies, SB1317 shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), oral bioavailability of 24%, ~4 and 37% in mice, rats, and dogs, respectively; and extensive tissue distribution in mice.
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• In Vitro:
  SB1317 (25 μM) has no inhibition of Human CYP1A2, 3A4, 2C9, and 2C19 isoforms, but has inhibition of CYP2D6 (IC50: 0.95 μM). SB1317 inhibits cell proliferation of HCT-116 (IC50: 0.079 μM) and HL-60 (IC50: 0.059 μM). SB1317 is mainly metabolized by CYP3A4 and CY1A2 in vitro. SB1317 does not inhibit any of the major human CYPs in vitro except CYP2D6 (IC50=1 μM). CYP1A and CYP3A4 are mainly expressed in human hepatocytes in vitro.
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Storage & Handling

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

Alternative Names

JAK2, FLT3, CDK2, SB1317 hydrochloride (1204918 72 8(free base)), SB1317 hydrochloride (1204918728(free base)), SB-1317 hydrochloride (1204918-72-8(free base)), SB1317 hydrochloride (1204918-72-8(free base)), TG02 Hydrochloride, TG-02 hydrochloride, TG-02 Hydrochloride, TG 02 Hydrochloride

Compound Identifiers

PubChem CID

141730164