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Darovasertib

PKC 抑制剂
规格或纯度: 99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
D413600-2mg
2mg 现货 Stock Image
D413600-5mg
5mg 现货 Stock Image
D413600-10mg
10mg 现货 Stock Image
D413600-25mg
25mg 现货 Stock Image
D413600-50mg
50mg 现货 Stock Image
D413600-100mg
100mg 现货 Stock Image

基本描述

规格或纯度 99%
英文名称 Darovasertib
别名 LXS-196;LXS196;IDE196
英文别名 LXS-196;LXS196;IDE196
生化机理 Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Information

Darovasertib (LXS-196) Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC) .


Targets

PKC

产品属性

ALogP 1.6
HBD Count 3
Rotatable Bond 5

名称和标识符

IUPAC Name 3-amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide
INCHI InChI=1S/C22H23F3N8O/c1-21(27)6-10-33(11-7-21)15-5-3-9-29-19(15)32-20(34)17-18(26)30-12-14(31-17)16-13(22(23,24)25)4-2-8-28-16/h2-5,8-9,12H,6-7,10-11,27H2,1H3,(H2,26,30)(H,29,32,34)
InChi Key XXJXHXJWQSCNPX-UHFFFAOYSA-N
Canonical SMILES CC1(CCN(CC1)C2=C(N=CC=C2)NC(=O)C3=NC(=CN=C3N)C4=C(C=CC=N4)C(F)(F)F)N
PubChem CID 118873253
分子量 472.47

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 60 mg/mL (126.99 mM); Ethanol: 20 mg/mL (42.33 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 22
DMSO(mM) Max Solubility 46.5638029927826
Water(mg / mL) Max Solubility <1

关联配体

Ligand ID 11186
名称 darovasertib
别名 LXS-196
类别 Synthetic organic
学名 3-amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Darovasertib (LXS196) is an oral protein kinase C (PKC) inhibitor that was developed by Novartis for antineoplastic potential. It is one of the chemical structures claimed in Novartis' patent WO2016020864A1 . Darovasertib is a potential first-in-class protein kinase C (PKC) inhibitor.
临床描述 This is a Phase 1/2, multi-center, open-label basket study designed to evaluate the safety and anti-tumor activity of IDE196 in patients with solid tumors harboring GNAQ or GNA11 (GNAQ/11) mutations or PRKC fusions, including metastatic uveal melanoma (MUM), cutaneous melanoma, colorectal cancer, and other solid tumors. Phase 1 (dose escalation) will assess safety, tolerability and pharmacokinetics of IDE196 via standard dose escalation scheme and determine the recommended Phase 2 dose. Safety and anti-tumor activity will be assessed in the Phase 2 (dose expansion) part of the study.
This study is to characterize the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD) and preliminary anti-tumor activity of LXS196 as a single agent and in combination with HDM201 in patients with metastatic uveal melanoma.
来源公司 IDEAYA Biosciences
Novartis

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