SGC0946|cas:1561178-17-3|西域试剂

SGC0946,99.68%

产品编号：Bellancom-15650| CAS NO：1561178-17-3| 分子式：C₂₈H₄₀BrN₇O₄| 分子量：618.57

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货号	价格	库存与货期
Bellancom-15650	￥990.00	杭州北京（现货）
Bellancom-15650	￥1575.00	杭州北京（现货）
Bellancom-15650	￥5880.00	杭州北京（现货）

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SGC0946

产品介绍

SGC0946 是一种选择性的 DOT1L (histone 3 lysine 79 methyltransferase) 抑制剂，其 IC₅₀ 值为 0.3 nM。SGC0946 可通过抑制 DOT1L，导致 G1 停滞以及抑制癌细胞的自我更新和转移潜力，诱导细胞分化。SGC0946 可用于白血病和乳腺癌的研究，也可作为探针以进一步研究 DOT1L 在正常和病变细胞中的细胞机制。

生物活性

SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC₅₀ of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells.

体外研究

SGC0946 (0-100 µM; 4 days) inhibits DOT1L with IC₅₀ of 2.65 nM in A431 cells.
SGC0946 (1, 5 µM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
SGC0946 (1 µM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation.
SGC0946 (1 µM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1.
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity.
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells.

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

Cell Viability Assay

Cell Line:	A431 cells
Concentration:	0-100 µM
Incubation Time:	4 days
Result:	Showed potent inhibitory activity against DOT1L with IC₅₀ of 2.65 nM in A431 cells.

Cell Viability Assay

Cell Line:	Human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
Concentration:	1, 5 µM
Incubation Time:	14 days
Result:	Killed human cord blood cells transformed with an MLL-AF9 fusion oncogene.

Western Blot Analysis

Cell Line:	Molm13 MLL cells
Concentration:	1 µM
Incubation Time:	3-7 days
Result:	Reduced H3K79me2 in Molm13 MLL cells in a time- and dose-dependent manner, and a complete inhibition exhibited at day 7.

Cell Proliferation Assay

Cell Line:	SK-OV-3 and TOV21G cells
Concentration:	0.2, 2, or 20 μM
Incubation Time:	12 days
Result:	Inhibited the growth of both SK-OV-3 and TOV21G cells in a dose- and time-dependent manner. Reduced the colony of both SK-OV-3 and TOV21G cells.

Cell Cycle Analysis

Cell Line:	SK-OV-3 and TOV21G cells
Concentration:	10 μM
Incubation Time:	12 days
Result:	Induced increased G1 population and decreased S phase and G2/M phase cells in asynchronized SK-OV-3 and TOV21G cells.

体内研究
(In Vivo)

SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors.

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

Animal Model:	Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model).
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice a week for 6 weeks.
Result:	Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group). Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

体内研究

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

Animal Model:	Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model).
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice a week for 6 weeks.
Result:	Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group). Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

体内研究

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

Animal Model:	Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model).
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice a week for 6 weeks.
Result:	Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group). Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.83 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6166 mL	8.0832 mL	16.1663 mL
5 mM	0.3233 mL	1.6166 mL	3.2333 mL
10 mM	0.1617 mL	0.8083 mL	1.6166 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。