GSK-3685032 - CAS:2170137-61-6

您当前的位置：

GSK-3685032

目录号 : KM8990 CAS No. : 2170137-61-6

Data Sheet 产品使用指南

GSK-3685032 是一种非时间依赖、非共价、可逆的 DNMT1 选择性抑制剂，IC₅₀=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Ginkgolide B In-stock
Isoginkgetin In-stock
Ginkgolic acid C17:1 In-stock
Ginkgolic Acid In-stock
Propargyl-PEG4-amine In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

体外研究

GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC₅₀ value of 0.64 μM.
GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC₅₀ throughout a 6 d time course.
GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription.
GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression.
GSK3685032 induces DNA hypomethylation and gene activation.

Cell Proliferation Assay

Cell Line:	15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells.
Concentration:	0.01-100 μM
Incubation Time:	6 days
Result:	Showed cell growth inhibition of majority cancer cell lines, with a median growth IC₅₀ value of 0.64 μM.

Cell Proliferation Assay

Cell Line:	MV4-11 cells
Concentration:	0.1-1000 nM
Incubation Time:	1-6 days
Result:	Exhibited growth inhibition after 3 days, with decreasing growth IC₅₀ throughout a 6 d time course.

RT-PCR

Cell Line:	MV4-11 cells
Concentration:	10-10000 nM
Incubation Time:	4 days
Result:	Dose-dependent increased of CXCL11, IFI27, HLA-DQA1 and MAGEA4 following treatment of MV4-11 cells.

Western Blot Analysis

Cell Line:	GDM-1 cells
Concentration:	3.2-10,000 nM
Incubation Time:	2 days
Result:	Inhibited DNMT1 protein expression

体内研究

GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models.

Summary of mouse pharmacokinetic parameters for GSK-3685032

Dose,Route	C_max (ng/mL)	AUC_0-8hr (h*ng/mL)	DNAUC (hkgng/mL/mg)	Clearance (mL/min/kg)	Volume_dss (L/kg)	T_1/2 (h)
2 mg/kg,IV	5103	2418	1209	13	1.3	1.8
2 mg/kg,SC	252	921	461	NA	NA	2.8
2 mg/kg,SC	5473	15400	513	NA	NA	ND

Animal Model:	MV4-11 xenograft models (female CD1-Foxn1 mice, 12 weeks of age) or SKM-1 xenograft models (NOD. CB17-Prkdc1NCrCrl mice, 8-11 weeks of age)
Dosage:	1, 5, 15, 30, 45 mg/kg (10% captisol adjusted to pH 4.5-5 with 1 M acetic acid, stored for up to 1 week at 4 °C)
Administration:	Subcutaneous injection, twice daily for 4 weeks
Result:	Revealed statistically significant dose-dependent tumor growth inhibition with clear regression at ≥30 mg/kg.

分子式

C₂₂H₂₄N₆Os

分子量

420.53

CAS号

2170137-61-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation