Fedratinib

ChemicalBook > CAS DataBase List > Fedratinib

Description In vitro In vivo

Product Name: Fedratinib
CAS No.: 936091-26-8
Chemical Name: Fedratinib
Synonyms: CS-57;TG-101348;SAR-302503;Fedratinib;Fedratinib D9;TG101348, >=98%;TG101348/TG-101348;SAR302503/TG101348;Fedratinib/TG101384;TG101348(Fedratinib)
CBNumber: CB12485002
Molecular Formula: C27H36N6O3S
Formula Weight: 524.68
MOL File: 936091-26-8.mol

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Fedratinib Property

Melting point:: 180-182°C
Boiling point:: 713.7±70.0 °C(Predicted)
Density: 1.247
storage temp.: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility: DMSO (Slightly), Methanol (Slightly)
form: Beige powder.
pka: 11.95±0.50(Predicted)
color: White to Off-White
CAS DataBase Reference: 936091-26-8

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Safety

HS Code: 29350090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16289
Product name: TG101348
Purity: ≥98%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 16289
Product name: TG101348
Purity: ≥98%
Packaging: 5mg
Price: $117
Updated: 2024/03/01

Cayman Chemical

Product number: 16289
Product name: TG101348
Purity: ≥98%
Packaging: 10mg
Price: $187
Updated: 2024/03/01

Cayman Chemical

Product number: 16289
Product name: TG101348
Purity: ≥98%
Packaging: 25mg
Price: $425
Updated: 2024/03/01

Usbiological

Product number: 169756
Product name: TG101348
Packaging: 1mg
Price: $282
Updated: 2021/12/16

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Fedratinib Chemical Properties,Usage,Production

Description

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35-and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

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. 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. 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.

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, at 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. Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo.

Uses

A potent, highly selective and ATP-competitive JAK2 inhibitor with an IC50 of 3 nM for JAK2 and JAK2V617F.

Uses

TG101348 is a selective inhibitor of JAK2 tyrosine kinase. Potent JAK2 inhibitor.

Definition

ChEBI: N-tert-butyl-3-[[5-methyl-2-[4-[2-(1-pyrrolidinyl)ethoxy]anilino]-4-pyrimidinyl]amino]benzenesulfonamide is a sulfonamide.

Biological Activity

tg101348, also known as sar302503, is a potent and selective inhibitor of janus kinase 2 (jak2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(jak1), jak2, janus kinase 3 (jak3) and tyrosine kinase 2 (tyk2), with the inhibition constant ic50 of 3 nm. comparing to other close related kinases, the selectivity of tg101348 for jak2 is 35- and 334-fold stronger than that for jak3 and jak1 respectively. tg10348 is capable of inducing apoptosis in hel cells as well baf/3 cells harboring jak2v617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (pv) patients.srdan verstovsek. therapeutic potential of jak2 inhibitors. hematology am soc hematol educ program 2009:636-642

target

JAK2

Fedratinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Fedratinib manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: Fedratinib(SAR302503, TG101348) 936091-26-8
Price: US $200.00-0.00/g
Min. Order: 10g
Purity: 98%+
Supply Ability: 100kgs
Release date: 2021-05-24

Career Henan Chemical Co

Product: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide 936091-26-8
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

936091-26-8, FedratinibRelated Search:

TG 100713 N,N-DIMETHYLHYDROXYLAMINE HYDROCHLORIDE N,N'-Dimethyl-1,3-propanediamine N,N-Dimethylbenzylamine N,N-Dimethylbenzamide N,N-Dimethylpropionamide 5-PYRIDIN-4-YL-1H-INDAZOLE 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol TG6-10-1 N-(tert-Butyl)-3-[[5-methyl-2-[[4-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide AZD 1480 TG101209 MK-2206 2HCl Momelotinib LY 294002 HYDROCHLORIDE Ruxolitinib

TG101348; TG 101348; TG-101348; SAR302503; SAR-302503; SAR 302503; FEDRATINIB.

TG101348(Fedratinib)

CS-57

TG-101348; TG 101348;SAR-302503;SAR 302503;SAR302503

TG 101348 - Fedratinib | SAR 302503

Fedratinib (SAR302503, TG101348), ≥98%

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide

TG-101348

N-TERT-BUTYL-3-(5-METHYL-2-(4-(2-(PYRROLIDIN-1-YL)ETHOXY)PHENYLAMINO)PYRIMIDIN-4-YLAMINO)BENZENESULFONAMIDE

SAR-302503

BenzenesulfonaMide, N-(1,1-diMethylethyl)-3-[[5-Methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-4-pyriMidinyl]aMino]-

TG101348 (SAR302503)

TG101348/TG-101348

SAR302503/TG101348

Fedratinib (SAR302503, TG101348)

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide TG 101348

Fedratinib (TG101348)

Fedratinib

TG101348, >=98%

Fedratinib/TG101384

FEDRATINIB (SAR302503, TG101348);TG101348;TG 101348

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl

Fedratinib (SAR302503)

Fedratinib(TG101348,SAR302503)

FEDRATINIB;SAR 302503;TG-101348;TG 101348

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide USP/EP/BP

N-tert-butyl-3-{[5-methyl-2-({4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}amino)pyrimidin-4-yl]amino}benzene-1-sulfonamide

n-(1,1-dimethylethyl)-3-((5-methyl-2-((4-(2-(1-pyrrolidinyl)...

Fedratinib D9

TG101348 Fedratinib SAR302503 TG-101348

Apoptosis,SAR-302503,STAT5,Inhibitor,Janus kinase,phosphorylation,FLT3,myeloproliferative,JAK2V617F,orally,SAR302503,inhibit,Fedratinib,anti-proliferation,JAK2,TG 101348,TG101348,JAK,RET,anti-cancer

Bazedoxifene Impurity 13

936091-26-8

C27H36N6O3S

Inhibitor

Inhibitors

JAK

STAT