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

Catalog No. T4227 CAS T4227

Synonyms: 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).

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

SB1317 hydrochloride (1204918-72-8(free base)), CAS T4227

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 63.00
5 mg	In stock	$ 115.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 340.00
50 mg	In stock	$ 413.00
100 mg	In stock	$ 615.00
1 mL * 10 mM (in DMSO)	In stock	$ 126.00

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Purity: 98.39%

Biological Description

Chemical Properties

Storage & Solubility Information

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	JAK2:73nM, FLT3:56 nM, CDK2:13nM
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
CAS No.	T4227

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 26.5 mg/mL

References and Literature

1. William AD, et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kina 2. Pasha MK, et al. PreClinicalal metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Epigenetics Compound Library Macrocyclic Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library

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Keywords

SB1317 hydrochloride (1204918-72-8(free base)) T4227 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors CDK JAK FLT TG02 Hydrochloride TG-02 hydrochloride SB1317 hydrochloride (1204918 72 8(free base)) SB-1317 hydrochloride (1204918-72-8(free base)) SB1317 hydrochloride (1204918728(free base)) TG-02 Hydrochloride TG 02 Hydrochloride inhibitor inhibit

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