1. Apoptosis
  2. Apoptosis
  3. SKLB-163

SKLB-163 是一种口服活性的 Rho GDP-dissociation (RhoGDI) 抑制剂。SKLB-163 抑制高表达的 RhoGDI 肿瘤细胞增殖和迁移,并增加肿瘤细胞的放射敏感性。SKLB-163 诱导癌细胞凋亡 (Apoptosis)。

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SKLB-163 Chemical Structure

SKLB-163 Chemical Structure

CAS No. : 1255099-06-9

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规格 价格 是否有货 数量
1 mg ¥2345
1 - 2 周
5 mg ¥5845
1 - 2 周
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
1.8 μM
Compound: 6t
Cytotoxicity against human A375 cells after 48 hrs by MTT assay
Cytotoxicity against human A375 cells after 48 hrs by MTT assay
[PMID: 21262571]
A-431 IC50
4.4 μM
Compound: 6t
Cytotoxicity against human A431 cells after 48 hrs by MTT assay
Cytotoxicity against human A431 cells after 48 hrs by MTT assay
[PMID: 21262571]
A549 IC50
4 μM
Compound: 6t
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 21262571]
BXPC-3 IC50
6.6 μM
Compound: 6t
Cytotoxicity against human BxPC3 cells after 48 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 48 hrs by MTT assay
[PMID: 21262571]
HCT-116 IC50
1.3 μM
Compound: 6t
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 21262571]
HeLa IC50
4.9 μM
Compound: 6t
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
[PMID: 21262571]
HepG2 IC50
1.1 μM
Compound: 6t
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 21262571]
MCF7 IC50
4.2 μM
Compound: 6t
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 21262571]
MDA-MB-468 IC50
4.1 μM
Compound: 6t
Cytotoxicity against human MDA-MB-468 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-468 cells after 48 hrs by MTT assay
[PMID: 21262571]
PC-3 IC50
6.1 μM
Compound: 6t
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
[PMID: 21262571]
SK-BR-3 IC50
8.8 μM
Compound: 6t
Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay
Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay
[PMID: 21262571]
SK-OV-3 IC50
4.8 μM
Compound: 6t
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay
[PMID: 21262571]
SW480 IC50
5.2 μM
Compound: 6t
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
[PMID: 21262571]
SW-620 IC50
1.2 μM
Compound: 6t
Cytotoxicity against human SW620 cells after 48 hrs by MTT assay
Cytotoxicity against human SW620 cells after 48 hrs by MTT assay
[PMID: 21262571]
体外研究
(In Vitro)

SKLB-163 (0-20 μM,48 小时) 抑制鼻咽癌 (NPC) 细胞的增殖和迁移,并使细胞对辐射敏感[1]
SKLB-163 (0-20 μM,48 h) 在 A375、SPC-A1、SW620、HeLa、PC-3 细胞中显示出细胞毒性作用[2]
SKLB-163 (0-2.5 μM,48 小时) 诱导 A375 细胞凋亡并抑制集落形成[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SKLB-163 (25-100 mg/kg,灌胃,每天一次,持续 30 天) 抑制鼻咽癌小鼠模型中肿瘤生长和腹水形成,并抑制肝和肺转移[1]
SKLB-163 (50 mg/kg,每天一次。从 SKLB-163 给药第 6 天开始,每天一次 3 Gy 辐射,持续 3 天) 使 CNE-2 和 C666-1 皮下异种移植小鼠模型中的 NPC 肿瘤对辐射敏感[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NPC lung metastatic model: transplanting NPC cells C666-1 into the livers of BALB/c nude mice[1]
Dosage: 25, 50, 100 mg/kg
Administration: intragastric administration, once daily for 30 days
Result: Reduced tumor size by 33.5% (25 mg/kg), 53.6% (50 mg/kg), 81.6% (100 mg/kg), respectively.
Ascited formation by 33.9% (25 mg/kg), 58.7% (50 mg/kg), 82.2% (100 mg/kg).
Inhibited liver or lung metastasis.
分子量

405.92

Formula

C18H16ClN3O2S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SKLB-163
目录号:
HY-120429
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