1. Cell Cycle/DNA Damage Apoptosis
  2. DNA/RNA Synthesis Apoptosis
  3. H3B-8800

H3B-8800 是一种有效的口服活性 SF3B 剪接 (SF3B splicing) 调节剂。H3B-8800 与 SF3b 复合物直接相互作用并显示出抗癌活性。H3B-8800 具有研究 SF3B1 突变体急性髓系白血病 (AML) 的潜力。

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H3B-8800 Chemical Structure

H3B-8800 Chemical Structure

CAS No. : 1825302-42-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant[1].

IC50 & Target

SF3B splicing[1]

体外研究
(In Vitro)

H3B-8800 (0.1-10000 nM; 72 h)抑制 SF3B1 突变细胞系 Panc05.04 细胞的生长[1]
H3B-8800 (0.1-10000 nM; 24 h) 以剂量依赖性方式诱导 SF3B1 突变细胞系 Panc05.04 细胞凋亡[1]

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

Apoptosis Analysis[1]

Cell Line: SF3B1-mutant cell line Panc05.04 cells
Concentration: 0.1,1, 10, 100, 1000, 10000 nM
Incubation Time: 24 h
Result: Induced apoptosis by increased caspase-3/7 cleavage in a dose-dependent manner.
体内研究
(In Vivo)

H3B-8800 (2, 4 mg/kg; p.o.; daily) 在具有 SF3B1 突变的 AML 衍生异种移植物 (PDX) 模型中显示出抗肿瘤活性[1]

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

Animal Model: 6-8 weeks, female NSG or CB17-SCID mice (K562 cells with SF3B1WT or SF3B1K700E)[1]
Dosage: 2, 4 mg/kg
Administration: P.o.; daily
Result: Resulted in antileukemic efficacy and splicing modulation in mice bearing AML patient-derived xenografts (PDXs) with a mutation in SF3B1 but had little effect in mice bearing SF3B1WT AML PDXs, significantly reduced leukemic burden relative in SF3B1K700E PDX.
分子量

555.71

Formula

C31H45N3O6

CAS 号
性状

固体

颜色

Yellow to orange

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (179.95 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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 1.7995 mL 8.9975 mL 17.9950 mL
5 mM 0.3599 mL 1.7995 mL 3.5990 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7995 mL 8.9975 mL 17.9950 mL 44.9875 mL
5 mM 0.3599 mL 1.7995 mL 3.5990 mL 8.9975 mL
10 mM 0.1799 mL 0.8997 mL 1.7995 mL 4.4987 mL
15 mM 0.1200 mL 0.5998 mL 1.1997 mL 2.9992 mL
20 mM 0.0900 mL 0.4499 mL 0.8997 mL 2.2494 mL
25 mM 0.0720 mL 0.3599 mL 0.7198 mL 1.7995 mL
30 mM 0.0600 mL 0.2999 mL 0.5998 mL 1.4996 mL
40 mM 0.0450 mL 0.2249 mL 0.4499 mL 1.1247 mL
50 mM 0.0360 mL 0.1799 mL 0.3599 mL 0.8997 mL
60 mM 0.0300 mL 0.1500 mL 0.2999 mL 0.7498 mL
80 mM 0.0225 mL 0.1125 mL 0.2249 mL 0.5623 mL
100 mM 0.0180 mL 0.0900 mL 0.1799 mL 0.4499 mL
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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产品名称:
H3B-8800
目录号:
HY-111517
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