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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $45 | In Stock | In Stock | |
| 2 mg | $63 | In Stock | In Stock | |
| 5 mg | $115 | In Stock | In Stock | |
| 10 mg | $189 | In Stock | In Stock | |
| 25 mg | $340 | In Stock | In Stock | |
| 50 mg | $413 | In Stock | In Stock | |
| 100 mg | $615 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $126 | In Stock | In Stock |
| 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. |
| Synonyms | TG-02 hydrochloride |
| Molecular Weight | 408.92 |
| Formula | C23H25ClN4O |
| Smiles | Cl.CN1C\C=C\CCOc2cccc(c2)-c2ccnc(Nc3cccc(C1)c3)n2 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (146.73 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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