(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-

Product Name: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-
CAS No.: 1421919-75-6
Chemical Name: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-
Synonyms: CS-1100;KPT-276;KPT276; KPT 276;KPT276, 10 mM in DMSO;(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-;(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- USP/EP/BP;(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one;(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one;2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)-;(KPT276)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
CBNumber: CB72680704
Molecular Formula: C16H10F8N4O
Formula Weight: 426.26
MOL File: 1421919-75-6.mol

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(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Property

Boiling point:: 477.2±55.0 °C(Predicted)
Density: 1.56±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in EtOH; insoluble in H2O; ≥19.85 mg/mL in DMSO
form: solid
pka: 0.59±0.50(Predicted)
color: White to off-white
InChI: InChI=1S/C16H10F8N4O/c17-14(18)6-27(7-14)12(29)1-2-28-8-25-13(26-28)9-3-10(15(19,20)21)5-11(4-9)16(22,23)24/h1-5,8H,6-7H2/b2-1-
InChIKey: JCHAWRDHMUSLMM-UPHRSURJSA-N
SMILES: C(N1CC(F)(F)C1)(=O)/C=C\N1C=NC(C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=N1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 29158
Product name: KPT-276
Packaging: 5mg
Price: $68
Updated: 2024/03/01

Cayman Chemical

Product number: 29158
Product name: KPT-276
Packaging: 10mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 29158
Product name: KPT-276
Packaging: 25mg
Price: $201
Updated: 2024/03/01

Cayman Chemical

Product number: 29158
Product name: KPT-276
Packaging: 50mg
Price: $268
Updated: 2024/03/01

ApexBio Technology

Product number: B1463
Product name: KPT-276
Packaging: 10mg
Price: $68
Updated: 2021/12/16

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(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Chemical Properties,Usage,Production

Description

KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity. In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.

Uses

PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE). PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1[1].

Synthesis

1333154-10-1

1421920-40-2

1421919-75-6

General synthesis of (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazole and compound (CAS:1421920-40-2) as raw material for (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one Procedure: to a 50 mL three-necked round-bottomed flask fitted with a nitrogen inlet under nitrogen protection was added 3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazole (0.18 g, 1.0 eq.) dissolved in DMF (5.0 mL, 27.0 V), followed by the addition of DABCO (0.143 g, 2.0 eq.) and (Z)-1-(3, 3-difluoroazetidin-1-yl)-3-iodo-2-en-1-one (0.192 g, 1.1 eq.). The reaction mixture was stirred at room temperature for 2-3 hours. The reaction progress was monitored by TLC using 80% ethyl acetate-hexane as the mobile phase with an Rf value of 0.60 for the feedstock and 0.4 for the product.Upon completion of the reaction, the mixture was poured into ice water (50 mL) and extracted with EtOAc (3 x 25 mL). The organic layers were combined, washed with brine solution (3 × 25 mL), dried over MgSO4, filtered, and concentrated by rotary evaporation (25 °C, 20 mmHg) to give 0.3 g of crude product. The crude product was purified by silica gel column chromatography (60/120 mesh) using ethyl acetate:hexane as mobile phase. The silica gel column (5 × 10 cm) was packed with hexane and then eluted with ethyl acetate in a gradient manner, starting from 40% ethyl acetate/hexane and gradually increasing to 45% ethyl acetate/hexane, and 50 mL of gradient was collected. The target compound was eluted starting from 40% ethyl acetate/hexane. The TLC distribution grade fractions containing the target compound were combined, resulting in 70 mg of pure product in 25.64% yield.

References

[1]. ranganathan p, yu x, na c, et al. preclinical activity of a novel crm1 inhibitor in acute myeloid leukemia. blood, 2012, 120(9): 1765-1773.
[2]. schmidt j, braggio e, kortuem km, et al. genome-wide studies in multiple myeloma identify xpo1/crm1 as a critical target validated using the selective nuclear export inhibitor kpt-276. leukemia, 2013, 27(12): 2357-2365.

(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Preparation Products And Raw materials

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(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Suppliers

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View Lastest Price from (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- manufacturers

Career Henan Chemical Co

Product: (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one 1421919-75-6
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-23

Career Henan Chemical Co

Product: (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one 1421919-75-6
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-20

1421919-75-6, (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-Related Search:

Selinexor 3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazole (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid 2-Propenoic acid, 3-iodo-, 1-methylethyl ester, (2Z)- (Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate PD 173074 KPT-330, (E)-RN Verdinexor (KPT-335) Bosutinib BIX 02189 Ribociclib KPT-185 Olaparib

(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-

KPT-276

2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)-

(KPT276)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one

KPT276; KPT 276

(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one

CS-1100

(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- USP/EP/BP

(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one

KPT276, 10 mM in DMSO

1421919-75-6

C16H10F8N4O

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Inhibitors