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安全性情報

適用法令

SML2628

NVP-BSK805 Trihydrochloride

Name: NVP-BSK805 Trihydrochloride
Brand: SIGMA

≥98% (HPLC)

別名:

4-(2,6-Difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine trihydrochloride, 8-(3,5-Difluoro-4-morpholin-4-ylmethyl-phenyl)-2-(1-piperidin-4-yl-1H-pyrazol-4-yl)-quinoxaline trihydrochloride, 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline trihydrochloride, BSK 805 3HCl, BSK805, 3HCl, NVP-BSK 805 3HCl

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About This Item

実験式（ヒル表記法）:

C₂₇H₂₈F₂N₆O·3HCl

CAS番号:

2320258-95-3

分子量:

599.93

MDL番号:

MFCD22419018

UNSPSCコード:

12352200

NACRES:

NA.77

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Sigma-Aldrich

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Supelco

D-160

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Y0001766

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Sigma-Aldrich

365831

5-フルオロ-2-ニトロベンゾトリフルオリド

アッセイ

≥98% (HPLC)

フォーム

powder

色

faint yellow to dark orange

溶解性

H₂O: 2 mg/mL, clear

保管温度

−20°C

SMILES記法

Fc1c(c(cc(c1)c3c4nc(cnc4ccc3)c5c[n](nc5)C6CCNCC6)F)CN2CCOCC2

InChI

1S/C27H28F2N6O/c28-23-12-18(13-24(29)22(23)17-34-8-10-36-11-9-34)21-2-1-3-25-27(21)33-26(15-31-25)19-14-32-35(16-19)20-4-6-30-7-5-20/h1-3,12-16,20,30H,4-11,17H2

InChI Key

IBPVXAOOVUAOKJ-UHFFFAOYSA-N

生物化学的／生理学的作用

NVP-BSK805 is a selective, ATP-competitive (Ki = 0.43 nM) Janus kinase 2 (JAK2) inhibitor (IC50 = 0.58 and 0.56 nM against full-length wild-type and V617F JAK2, respectively) with greatly reduced potency against TYK2, JAK3, JAK1 (IC50 = 10.76, 18.68, 31.63 nM against respective JAK homology domain 1) and >300-fold selectivity over a panel of 36 other kinases. BSK805 potently inhibits STAT5 phosphorylation (by >90% at 100 nM; MB-02 & SET-2 cells) and proliferation in JAK2V617F mutant cultures in vitro (GI50= 39-331 nM; 75% SET-2 growth inhibition at 150 nM) and in Ba/F3 JAK2V617F-bearing mice in vivo (150 mg/kg p.o.). BSK805 daily oral administration is also efficacious against rhEpo-induced splenomegaly and polycythemia in mice (50-100 mg/kg) and rats (25-50 mg/kg) with good pharmacokinetics and oral avilability.

Orally available, ATP-competitive Janus kinase 2 (JAK2) inhibitor with efficacy against JAK2V617F-driven leukemic disease in mice and rats in vivo.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML2628-VAR:
SML2628-BULK:
SML2628-25MG:
SML2628-5MG:

最新バージョンのいずれかを選択してください：

試験成績書（COA）

Lot/Batch Number

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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine.

Ji Hyun Cheon et al.

Biochemical and biophysical research communications, 490(4), 1176-1182 (2017-07-04)

P-glycoprotein (P-gp) is overexpressed in cancer cells in order to pump out chemotherapeutic drugs, and is one of the major mechanisms responsible for multidrug resistance (MDR). It is important to identify P-gp inhibitors with low toxicity to normal cells in

Tumor-associated GM-CSF overexpression induces immunoinhibitory molecules via STAT3 in myeloid-suppressor cells infiltrating liver metastases.

M Thorn et al.

Cancer gene therapy, 23(6), 188-198 (2016-05-21)

Assumptions that liver immune cells and immunosuppressive pathways are similar to their counterparts in other spaces have led to gaps in our understanding of intrahepatic neoplasm aggressiveness. Myeloid-derived suppressor cells (MDSCs) are potent inhibitors of antitumor immunity and pose a

Triple-negative breast cancers with amplification of JAK2 at the 9p24 locus demonstrate JAK2-specific dependence.

Justin M Balko et al.

Science translational medicine, 8(334), 334ra53-334ra53 (2016-04-15)

Amplifications at 9p24 have been identified in breast cancer and other malignancies, but the genes within this locus causally associated with oncogenicity or tumor progression remain unclear. Targeted next-generation sequencing of postchemotherapy triple-negative breast cancers (TNBCs) identified a group of

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Carole Pissot-Soldermann et al.

Bioorganic & medicinal chemistry letters, 20(8), 2609-2613 (2010-03-17)

We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compounds from this series

Spatial Proximity to Fibroblasts Impacts Molecular Features and Therapeutic Sensitivity of Breast Cancer Cells Influencing Clinical Outcomes.

Andriy Marusyk et al.

Cancer research, 76(22), 6495-6506 (2016-11-05)

Using a three-dimensional coculture model, we identified significant subtype-specific changes in gene expression, metabolic, and therapeutic sensitivity profiles of breast cancer cells in contact with cancer-associated fibroblasts (CAF). CAF-induced gene expression signatures predicted clinical outcome and immune-related differences in the

主要文書

安全性情報

NVP-BSK805 Trihydrochloride

≥98% (HPLC)

About This Item

おすすめの製品

特性

アッセイ

フォーム

色

溶解性

保管温度

SMILES記法

InChI

InChI Key

詳細

生物化学的／生理学的作用

安全性情報

保管分類コード

WGK

引火点(°F)

引火点(℃)

適用法令

Jan Code

資料

試験成績書（COA）

以前この製品を購入いただいたことがある場合

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