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354812-17-2生产厂家

354812-17-2价格

354812-17-2

354812-17-2结构式
354812-17-2结构式

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中文名 4-氨基-[2,3']联噻吩-5-甲酰胺
英文名 3-amino-5-thiophen-3-ylthiophene-2-carboxamide
英文别名 4-Amino-2,3'-bithiophene-5-carboxamide
[2,3'-Bithiophene]-5-carboxamide, 4-amino-
4-Amino-[2,3"]bithiophenyl-5-carboxylic acid amide
SC-514
IKK-2 Inhibitor
GK 01140
描述 SC-514 是一种选择性 IKK-2 抑制剂 (IC50=11.2±4.7 μM),不抑制其他 IKK 亚型或其他丝氨酸-苏氨酸和酪氨酸激酶。
相关类别
靶点

IKK-2:11.2 μM (IC50)

CDK2/A:61 μM (IC50)

AUR2:71 μM (IC50)

PRAK:75 μM (IC50)

MSK:123 μM (IC50)

体外研究 SC-514抑制天然IKK复合物或重组人IKK-1/IKK-2异二聚体,IC50分别为6.1±2.2μM和2.7±0.7μM。 SC-514对IKK-2的抑制具有选择性,可逆性和ATP竞争性。 SC-514以剂量依赖性方式抑制IL-1β诱导的类风湿性关节炎衍生的滑膜成纤维细胞中NF-κB依赖性基因的转录。 SC-514抑制所有形式的重组人IKK-2,包括rhIKK-2同源二聚体,rhIKK-1/rhIKK-2异二聚体,以及组成型活性形式的rhIKK-2,IC50值在3-12μM范围内相当[ 1]。评估活性氧(ROS)诱导IKKβ抑制剂是否增加黑素瘤细胞对亚硝基脲的敏感性。首先将黑素瘤细胞的反应评估为SC-514/Fotemustine共处理。将黑素瘤细胞系用50μM的SC-514和福莫司汀单独处理并组合处理48小时并评估生长抑制。与SC-514共同处理显着增强了Fotemustine诱导的所有黑素瘤细胞系的细胞毒性[2]。
体内研究 SC-514在炎症的急性模型中是有效的,即在大鼠中LPS诱导的血清TNFα产生。 SC-514显示TNFα产生的剂量依赖性抑制,证实IKK-2是体内潜在的抗炎药物靶标[1]。为了获得SC-514在癌细胞对Fotemustine的反应中的暗示的体内证据,使用黑素瘤的异种移植小鼠模型。用载体对照和25mg/kg SC-514和/或25mg/kg Fotemustine每天处理移植有A375或G361肿瘤的裸鼠连续13-15天,并监测肿瘤行为。用SC-514进行福莫司汀治疗显示出明显的联合作用,并减少了小鼠肿瘤的大小[2]。
激酶实验 使用NEMO抗体(3-10μg)从IL-1β处理的RASF细胞裂解物(0.5-2mg)免疫沉淀IKK复合物,然后加入蛋白A-琼脂糖珠。通过离心沉淀抗体复合物,并用1mL冷全细胞裂解缓冲液洗涤3次,然后在激酶缓冲液(25mM HEPES,pH 7.6,2mM MgCl 2,2mM MnCl 2,10mM NaF,5mM DTT)中洗涤2次。和1mM苯甲基磺酰氟)。在含有10μM生物素化的IκBα肽作为底物和1μM[γ-33P] ATP(2500Ci / mmol)的反应中分析100-200μg免疫沉淀的IKK的激酶活性。在室温下孵育30分钟后,取出25μL反应混合物并加入到SAM96生物素捕获板中。在连续洗涤步骤后,使板空气干燥,并向每个孔中加入25μL闪烁液。使用Top-Count NXT [1]测量[γ-33P] ATP的掺入。
细胞实验 对于结晶紫染色测定,将黑素瘤细胞系(1×104)接种在60mm培养皿中,然后未处理或用SC-514(50μM)和/或福莫司汀预处理。然后,将细胞用福尔马林固定并用结晶紫染色。细胞数测量为来自福尔马林固定细胞的溶解的结晶紫在595nm处的光密度(OD595)。细胞毒性也通过MTT还原试验确定[2]。
动物实验 通过口服管饲法(50mg / kg)或腹膜内(10和50mg / kg)给已经被剥夺食物过夜的成年雄性Wistar大鼠施用大鼠[1] SC-514或载体(2%Me2SO的盐水溶液)。 。化合物处理2小时后,在LPS给药后90分钟腹膜内给予盐水中1mg / kg LPS(大肠杆菌);将动物放血并通过大鼠特异性TNFαELISA分析血清TNFα水平。小鼠[2]将雄性nu / nu BALB / c小鼠(6周龄)保持在单独的通风笼中。将A375或G361(5×106)细胞重悬于0.1mL PBS中并皮下接种到裸鼠背部并使其生长7天。之后,将小鼠随机分配到4组(每组n = 6)并通过腹膜内注射200μL30%PEG / 5%吐温-80溶液作为媒介物对照和25mg / kg SC-514和/或或每天25 mg / kg Fotemustine连续13-15天。每3天测量体重和肿瘤体积。通过卡尺确定肿瘤体积并计算。在实验结束时,处死小鼠并收集肿瘤异种移植物。将肿瘤组织储存在-80℃下用于Western印迹分析。
参考文献

[1]. Kishore N, et al. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71.

[2]. Tse AK, et al. Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. Redox Biol. 2017 Apr;11:562-576.

密度 1.5±0.1 g/cm3
沸点 399.2±42.0 °C at 760 mmHg
熔点 209-211°C
分子式 C9H8N2OS2
分子量 224.303
闪点 195.2±27.9 °C
精确质量 224.007797
PSA 125.59000
LogP 1.52
外观性状 white to light brown
蒸汽压 0.0±0.9 mmHg at 25°C
折射率 1.715
储存条件 Store at +4°C
水溶解性 DMSO: soluble10mg/mL, clear

SECTION 1: Identification of the substance/mixture and of the company/undertaking
Product identifiers
Product name: SC-514
REACH No.: A registration number is not available for this substance as the substance
or its uses are exempted from registration, the annual tonnage does not
require a registration or the registration is envisaged for a later
registration deadline.
CAS-No.: 354812-17-2
Relevant identified uses of the substance or mixture and uses advised against
Identified uses: Laboratory chemicals, Manufacture of substances



SECTION 2: Hazards identification
Classification of the substance or mixture
Classification according to Regulation (EC) No 1272/2008
Acute toxicity, Oral (Category 3), H301
For the full text of the H-Statements mentioned in this Section, see Section 16.
Classification according to EU Directives 67/548/EEC or 1999/45/EC
T ToxicR25
For the full text of the R-phrases mentioned in this Section, see Section 16.
Label elements
Labelling according Regulation (EC) No 1272/2008
Pictogram
Signal wordDanger
Hazard statement(s)
H301Toxic if swallowed.
Precautionary statement(s)
P301 + P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/
physician.
Supplemental Hazardnone
Statements
Other hazards - none

SECTION 3: Composition/information on ingredients
Substances
Synonyms: 4-Amino-[2,3"]bithiophenyl-5-carboxylic acid amide
Formula: C9H8N2OS2
Molecular Weight: 224,3 g/mol
CAS-No.: 354812-17-2
Hazardous ingredients according to Regulation (EC) No 1272/2008
ComponentClassificationConcentration
SC-514
CAS-No.354812-17-2Acute Tox. 3; H301<= 100 %
Hazardous ingredients according to Directive 1999/45/EC
ComponentClassificationConcentration
SC-514
CAS-No.354812-17-2T, R25<= 100 %
For the full text of the H-Statements and R-Phrases mentioned in this Section, see Section 16

SECTION 4: First aid measures
Description of first aid measures
General advice
Consult a physician. Show this safety data sheet to the doctor in attendance.
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician.
In case of skin contact
Wash off with soap and plenty of water. Take victim immediately to hospital. Consult a physician.
In case of eye contact
Flush eyes with water as a precaution.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.
Most important symptoms and effects, both acute and delayed
The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in
section 11
Indication of any immediate medical attention and special treatment needed
no data available

SECTION 5: Firefighting measures
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, nitrogen oxides (NOx), Sulphur oxides
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

SECTION 6: Accidental release measures
Personal precautions, protective equipment and emergency procedures
Wear respiratory protection. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure
adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust.
For personal protection see section 8.
Environmental precautions
Prevent further leakage or spillage if safe to do so. Do not let product enter drains.
Methods and materials for containment and cleaning up
Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed
containers for disposal.
Reference to other sections
For disposal see section 13.

SECTION 7: Handling and storage
Precautions for safe handling
Avoid contact with skin and eyes. Avoid formation of dust and aerosols.
Provide appropriate exhaust ventilation at places where dust is formed.
For precautions see section 2.2.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Recommended storage temperature: 2 - 8 °C
Specific end use(s)
A part from the uses mentioned in section 1.2 no other specific uses are stipulated

SECTION 8: Exposure controls/personal protection
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
Avoid contact with skin, eyes and clothing. Wash hands before breaks and immediately after handling
the product.
Personal protective equipment
Eye/face protection
Face shield and safety glasses Use equipment for eye protection tested and approved under
appropriate government standards such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
Complete suit protecting against chemicals, The type of protective equipment must be selected
according to the concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
Where risk assessment shows air-purifying respirators are appropriate use a full-face particle
respirator type N99 (US) or type P2 (EN 143) respirator cartridges as a backup to engineering
controls. If the respirator is the sole means of protection, use a full-face supplied air respirator. Use
respirators and components tested and approved under appropriate government standards such
as NIOSH (US) or CEN (EU).
Control of environmental exposure
Prevent further leakage or spillage if safe to do so. Do not let product enter drains.

SECTION 9: Physical and chemical properties
Information on basic physical and chemical properties
a) AppearanceForm: solid
b) Odourno data available
c) Odour Thresholdno data available
d) pHno data available
e) Melting point/freezingno data available
point
f) Initial boiling point and no data available
boiling range
g) Flash pointno data available
h) Evapouration rateno data available
i) Flammability (solid, gas) no data available
j) Upper/lowerno data available
flammability or
explosive limits
k) Vapour pressureno data available
l) Vapour densityno data available
m) Relative densityno data available
n) Water solubilityno data available
o) Partition coefficient: n- log Pow: 1,055
octanol/water
p) Auto-ignitionno data available
temperature
q) Decompositionno data available
temperature
r) Viscosityno data available
s) Explosive propertiesno data available
t) Oxidizing propertiesno data available
Other safety information
no data available

SECTION 10: Stability and reactivity
Reactivity
no data available
Chemical stability
Stable under recommended storage conditions.
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
no data available
Hazardous decomposition products
In the event of fire: see section 5

SECTION 11: Toxicological information
Information on toxicological effects
Acute toxicity
no data available
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitisation
no data available
Germ cell mutagenicity
no data available
Carcinogenicity
IARC:No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Additional Information
RTECS: Not available
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.

SECTION 12: Ecological information
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
PBT/vPvB assessment not available as chemical safety assessment not required/not conducted
Other adverse effects
no data available

SECTION 13: Disposal considerations
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company. Dissolve or mix the material
with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber.
Contaminated packaging
Dispose of as unused product.

SECTION 14: Transport information
UN number
ADR/RID: 2811IMDG: 2811IATA: 2811
UN proper shipping name
ADR/RID: TOXIC SOLID, ORGANIC, N.O.S. (SC-514)
IMDG: TOXIC SOLID, ORGANIC, N.O.S. (SC-514)
IATA:Toxic solid, organic, n.o.s. (SC-514)
Transport hazard class(es)
ADR/RID: 6.1IMDG: 6.1IATA: 6.1
Packaging group
ADR/RID: IIIIMDG: IIIIATA: III
Environmental hazards
ADR/RID: noIMDG Marine pollutant: noIATA: no
Special precautions for user
no data available



SECTION 15 - REGULATORY INFORMATION
N/A


SECTION 16 - ADDITIONAL INFORMATION
N/A
符号 GHS06
GHS06
信号词 Danger
危害声明 H301
警示性声明 P301 + P310
危害码 (欧洲) T
风险声明 (欧洲) 25
安全声明 (欧洲) 45
危险品运输编码 UN 2811 6.1 / PGIII
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