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Merck
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文件

SML2589

Sigma-Aldrich

达沙替尼

≥98% (HPLC), powder, protein kinases inhibitor

别名:

BMS 354825, BMS-354825, BMS354825, N-(2-氯-6-甲基苯基)-2-[[6-[4-(2-羟乙基)-1-哌嗪基]-2-甲基-4-嘧啶基]氨基]-5-噻唑甲酰胺

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About This Item

经验公式（希尔记法）:
C22H26ClN7O2S
CAS号:
302962-49-8
分子量:
488.01
MDL號碼:
MFCD11046566
分類程式碼代碼:
12352200
NACRES:
NA.77

product name

达沙替尼, ≥98% (HPLC)

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCO)=N1

InChI

1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)

InChI 密鑰

ZBNZXTGUTAYRHI-UHFFFAOYSA-N

基因資訊

human ... ABL1(25) , BLK(640) , EPHA2(1969) , FGR(2268) , FRK(2444) , FYN(2534) , HCK(3055) , KIT(3815) , LCK(3932) , LYN(4067) , PDGFRB(5159) , SRC(6714) , SRMS(6725) , YES1(7525)

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應用

达沙替尼已用于：
  • 作为蛋白激酶抑制剂用于研究其对大鼠巨噬细胞极化、脂肪生成、西方饮食诱导的单纯性脂肪变性向脂肪肝（NASH）的进展以及肝纤维化的作用
  • 作为SRC酪氨酸激酶抑制剂用于研究其对肝细胞癌细胞的作用
  • 作为酪氨酸激酶抑制剂用于研究其对神经细胞自噬的作用。

生化／生理作用

达沙替尼是一种噻唑甲酰胺化合物，可抑制各种蛋白激酶，如裂点簇区-酪氨酸蛋白激酶ABL（Bcr-Abl）、Btk 家族成员、血小板衍生生长因子受体α/β（PDGFR-α/β）和肝配蛋白受体激酶。它也抑制Src 家族激酶，如SRC酪氨酸激酶和淋巴细胞特异性蛋白激酶（LCK）。达沙替尼对造血细胞有某些作用，如抑制自然杀伤细胞毒性、抑制T淋巴细胞活化和增殖，影响血小板活化。它也用于研究慢性粒细胞白血病（CML）和急性淋巴细胞白血病（ALL）的治疗。

訊號詞

Danger

危險分類

Aquatic Chronic 1 - Carc. 2 - Eye Dam. 1 - Repr. 2 - Skin Irrit. 2 - STOT RE 1

標靶器官

Gastro-intestinal system

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Hassan Reda Hassan Elsayed et al.
Annals of anatomy = Anatomischer Anzeiger : official organ of the Anatomische Gesellschaft, 234, 151626-151626 (2020-11-05)
Non-alcoholic fatty liver disease (NAFLD) is a worldwide disease that progresses into steatohepatitis (NASH) that has no current effective treatment. This study aimed, for the first time, to investigate the effect of Dasatinib; a tyrosine kinase inhibitor showing anti-PDGFR activity
Khushwant S Bhullar et al.
Food chemistry. Molecular sciences, 4, 100069-100069 (2022-04-14)
Dasatinib, a small-molecule drug used as a treatment for chronic myeloid leukemia induces mitochondrial damage in embryonic kidney (293 T) cells (p < 0.05). This dasatinib induced mitochondrial injury in kidney cells was mitigated by H3K36me3 activating ovotransferrin-derived peptides GWN and GW. Pre-treatment
Hassan Reda Hassan Elsayed et al.
Cells, 11(4) (2022-02-26)
Obesity causes renal changes (ORC), characterized by defective renal autophagy, lipogenesis, enhanced macrophage infiltration and apoptosis. We hypothesize that Dasatinib, a tyrosine kinase inhibitor, may ameliorate changes associated with obesity. We the mice with either Obesogenic diet (OD) or a
Liat Bar-On et al.
PloS one, 18(12), e0294176-e0294176 (2023-12-27)
SARS-CoV-2 infection elicits robust CD8 T-cell responses, yet the identity of the mechanisms playing dominant roles in initiating the virus-specific CD8 T-cell responses are largely unknown. In the present study, we interrogate the contribution of the cDC1 subset to SARS-CoV-2-specific
Markus Lindauer et al.
Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer, 212, 29-68 (2018-08-03)
Dasatinib is an oral available short-acting inhibitor of multiple tyrosine kinases. It was designed to inhibit ABL and SRC, but also has activity in multiple other kinases, including c-KIT, PDGFR-α, PDGFR-β, and ephrin receptor kinases. Dasatinib is a very potent inhibitor
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