BIX-01294 - CAS:935693-62-2

您当前的位置：

BIX-01294

目录号 : KM2665 CAS No. : 935693-62-2 纯度 : 98%

产品说明书产品使用指南

BIX-01294 是一种可逆且高度选择性的 G9a 组蛋白甲基转移酶抑制剂，在 DELFIA 试验中的 IC₅₀ 为 2.7 μM。BIX-01294 特异性抑制 G9a (H3K9me2) 和 GLP (H3K9me3)，IC₅₀s 分别为 1.7 μM 和 38 μM。BIX-01294 通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。BIX-01294 是一种 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物，可诱导坏死性凋亡 (necroptosis) 和自噬。BIX-01294 在复发性肿瘤细胞中具有抗肿瘤活性。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Lamotrigine-d3 In-stock
Apatinib-d8 In-stock
BRD5631 In-stock
AMDE-1 In-stock
MDK-6983 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

BIX-01294 is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC₅₀ of 2.7 μM in DELFIA assay. BIX-01294 specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC₅₀s of 1.7 μM and 38 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.

体外研究

BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth.
BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL.
BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.
BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.
BIX-01294 leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h).
BIX-01294 (4.1 μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells.
BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM).
BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF.

Cell Viability Assay

Cell Line:	Primary or recurrent tumor cells
Concentration:	2 μM
Incubation Time:	48 hours
Result:	Selectively inhibited recurrent tumor cell growth.

体内研究

BIX-01294 (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited.

Animal Model:	Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells
Dosage:	10 mg/kg
Administration:	IP; three times a week for 2 weeks
Result:	Significantly reduced tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.

分子式

C₂₈H₃₈N₆O₂

分子量

490.64

CAS号

935693-62-2

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

溶解性数据

In Vitro:

DMSO : ≥ 110 mg/mL (224.20 mM)

H₂O : 1 mg/mL (2.04 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0382 mL	10.1908 mL	20.3815 mL
5 mM	0.4076 mL	2.0382 mL	4.0763 mL
10 mM	0.2038 mL	1.0191 mL	2.0382 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: ≥ 2.75 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.60 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 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。