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Telaglenastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telaglenastat图片
CAS NO:1439399-58-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
CB-839
产品介绍
Telaglenastat (CB-839) 是一种首创的,选择性的,可逆性的,口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat 抑制GLS1剪接变异体KGAGAC,比 GLS2 具有更高的选择性。Telaglenastat 对小鼠类肾和脑中的内源性谷氨酰胺酶的IC50值分别为 23 nM 和 28 nM。Telaglenastat 还可诱导细胞自噬 (autophagy),并具有强大的抗肿瘤活性。
生物活性

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally activeglutaminase1 (GLS1)inhibitor. Telaglenastat selectively inhibitsGLS1splice variantsKGA (kidney-type glutaminase)andGAC (glutaminase C)compared to GLS2. TheIC50s are 23 nM and 28 nM for endogenousglutaminasein mouse kidney and brain, respectively. Telaglenastat inuducesautophagyand has antitumor activity[1].

IC50& Target

IC50: 23 nM (GLS1 in kidney), 28 nM (GLS1 in brain), >1 μM (GLS2 in liver)[1]

体外研究
(In Vitro)

Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively[1].
Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1].

Cell Proliferation Assay[1]

Cell Line:HCC1806, MDA-MB-231 cells
Concentration:0.1, 1, 10, 100, 1000 nM
Incubation Time:72 hours
Result:Has a potent effect on the proliferation of the two TNBC cell lines (IC50of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells).

Apoptosis Analysis[1]

Cell Line:MDA-MB-231, HCC1806 cells
Concentration:1 μM
Incubation Time:72 hours
Result:Caspase 3/7 activation.
体内研究
(In Vivo)

Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].

Animal Model:Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)[1]
Dosage:200 mg/kg
Administration:Oral administration; twice daily for 28 days
Result:Suppressed tumor growth by 61% relative to vehicle control at the end of study.
Clinical Trial
分子量

571.57

性状

Solid

Formula

C26H24F3N7O3S

CAS 号

1439399-58-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 6.29 mg/mL(11.00 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7496 mL8.7478 mL17.4957 mL
5 mM0.3499 mL1.7496 mL3.4991 mL
10 mM0.1750 mL0.8748 mL1.7496 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: 20%HP-β-CD/10 mM citrate pH 2.0

    Solubility: 10 mg/mL (17.50 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 20%SBE-β-CD/10 mM Trisodium citrate adjusted to pH 2.0 with HCL

    Solubility: 5 mg/mL (8.75 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1M HCl and heat to 55℃

  • 3.

    请依序添加每种溶剂: 70%PEG300   30% (20%SBE-β-CDin saline)

    Solubility: 4 mg/mL (7.00 mM); Suspended solution; Need ultrasonic and warming and heat to 55℃

*以上所有助溶剂都可在本网站选购。