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

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Catalog No. T4227
Alias TG-02 hydrochloride

SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).

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

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

🥰Excellent
Purity: 99.84%
Catalog No. T4227Alias TG-02 hydrochloride
SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
Pack SizePriceAvailabilityQuantity
1 mg$45In Stock
2 mg$63In Stock
5 mg$115In Stock
10 mg$189In Stock
25 mg$340In Stock
50 mg$413In Stock
100 mg$615In Stock
1 mL x 10 mM (in DMSO)$126In Stock
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Purity:99.84%
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Product Introduction

Bioactivity
Description
SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
Targets&IC50
CDK2:13nM, JAK2:73nM, FLT3:56 nM
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)[1]. 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.
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[1]. 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.
AliasTG-02 hydrochloride
Chemical Properties
Molecular Weight408.92
FormulaC23H25ClN4O
SmilesCl.CN1C\C=C\CCOc2cccc(c2)-c2ccnc(Nc3cccc(C1)c3)n2
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (146.73 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4455 mL12.2273 mL24.4547 mL122.2733 mL
5 mM0.4891 mL2.4455 mL4.8909 mL24.4547 mL
10 mM0.2445 mL1.2227 mL2.4455 mL12.2273 mL
20 mM0.1223 mL0.6114 mL1.2227 mL6.1137 mL
50 mM0.0489 mL0.2445 mL0.4891 mL2.4455 mL
100 mM0.0245 mL0.1223 mL0.2445 mL1.2227 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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