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Signaling Pathway

TG-101348

HY-10409

(Fedratinib; SAR 302503; TG101348; TG 101348)

TG-101348

TG-101348 Chemical Structure

TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.

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10 mM * 1 mL in DMSO $121 In-stock
10 mg $110 In-stock
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10 mM * 1 mL in DMSO €119 In-stock
10 mg €108 In-stock
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100 mg €556 In-stock
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Product name: TG-101348
Cat. No.: HY-10409

TG-101348 Data Sheet

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    Purity: 99.70%

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Related Compound Libraries

Compare The Inhibitor Activity of JAK ( IC50 or Ki Value )

Compound Name Bcl-2 Bcl-B Bcl-w ...
ABT-737 30.3 nM  
ABT-263 ≤1 nM, Ki ≤1 nM, Ki  
Obatoclax 3 uM  
...        
Full Table

Biological Activity of TG-101348

TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.
IC50 value: 3 nM (JAK2); 340 nM (BRD4) [1] [4]
Target: JAK2; BRD4
in vitro: TG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG101348 has an IC50 ~300-fold higher for the closely related JAK3 and is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with IC50 of 305 nM and 270 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. TG101348 does not show proapoptotic activity in control normal human dermal fibroblasts at concentrations up to 10 μM, and the antiproliferative IC50 against fibroblasts is >5 μM [1]. TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation [2]. TG101348 inhibits the proliferation of HMC-1.1 (KITV560G) cells, with somewhat lower potency than HMC-1.2 (KITD816V, KITV560G) cells, with IC50 of 740 nM and 407 nM, respectively [3]. TG101348 also is a inhibitor of BRD4 with IC50 of 340 nM [4].
in vivo: TG101348 has potential for efficacious treatment of JAK2V617F-associated myeloproliferative diseases (MPD). In treated animals, there is a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis, and, t least in some instances, evidence for attenuation of myelofibrosis, correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction. There are no apparent toxicities and no effect on T cell number [1]. Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo [2].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 524.68 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C27H36N6O3S
CAS No 936091-26-8
Solvent & Solubility

DMSO:42mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.9059 mL 9.5296 mL 19.0592 mL
5 mM 0.3812 mL 1.9059 mL 3.8118 mL
10 mM 0.1906 mL 0.9530 mL 1.9059 mL

Clinical Information of TG-101348

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
TG-101348 Sanofi Polycythemia vera 30-NOV-12 30-JUN-14 Phase 2 09-NOV-13
Sanofi Myelofibrosis 30-APR-12 30-SEP-19 Phase 2 07-OCT-13
Sanofi Myelofibrosis 31-DEC-11 31-MAR-16 Phase 3 13-NOV-13
Sanofi Myelofibrosis 30-NOV-12 30-JUN-14 Phase 2 09-NOV-13
Sanofi Thrombocythemia 30-NOV-12 30-JUN-14 Phase 2 09-NOV-13
Sanofi Myelofibrosis 31-AUG-11 31-JAN-14 Phase 2 26-AUG-13

References on TG-101348

Inhibitor Kit

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Compound Name Bcl-2 Bcl-B Bcl-w Bcl-xL Mcl-1 Bfl-1 Other target Note
ABT-737 30.3 nM 78.7 nM 197.8 nM
ABT-263 ≤1 nM, Ki ≤1 nM, Ki ≤0.5 nM, Ki
Obatoclax 3 uM 2.9 uM 5 uM
TW-37 290 nM Ki 1110 nM, Ki 360 nM, Ki
ABT-199 10 nM, Ki >10 uM, Ki >10 uM, Ki No inhibition Bcl-2 selective
AT101 320 nM, Ki 480 nM, Ki 180 nM, Ki
HA14-1 9 uM
Gambogic Acid 1.21 uM 0.66 uM 2.02 uM 1.47 uM 0.79 uM 1.06 uM Caspase
(+)-Apogossypol 0.5-2 uM 0.5-2 uM 0.5-2 uM 0.5-2 uM 0.5-2 uM No inhibition
Mcl1-IN-1 No inhibition 2.4 uM Mcl1 selective
MIM1 >50 uM 4.8 uM Mcl1 selective
Pyridoclax 25 nM, Kd