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Pan-RAS-IN-1 Sale

目录号 : GC32716

Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.

Pan-RAS-IN-1 Chemical Structure

Cas No.:1835283-94-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,790.00
现货
1mg
¥513.00
现货
5mg
¥1,134.00
现货
10mg
¥1,764.00
现货
25mg
¥3,528.00
现货
50mg
¥5,292.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.

[1] Welsch ME, et al. Multivalent Small-Molecule Pan-RAS Inhibitors. Cell. 2017 Feb 23;168(5):878-889.e29.

实验参考方法

Cell experiment:

For 384-well cancer cell viability assays, cells are trypsinized, counted, and seeded into 384-well plates at 1,000 cells/well. After 16 hr, pan-RAS-IN-1 (from 10 mM stocks in DMSO) are arrayed in an 8-point or 16-point dilution series in 384-well polypropylene plates. Compound solutions are transferred at a 1:5 dilution into the assay plates. After 48 hr, a 50% Alamar blue solution is added to a final concentration of 10% Alamar blue. After 6 hr of incubation, fluorescence intensity is determined at 535 and 590 nm[1].

Animal experiment:

Mice: Mice tumor Xenograft are dosed with 180 mg/kg pan-RAS-IN-1 orally (12 mg/mL, 10% DMSO, pH 4), vehicle orally, or by a combination of i.p. and i.v. injections at 30 mg/kg (4 mg/mL, 5% DMSO in HBSS at pH 4). Over 14 d, mice receive a total of 10 doses of pan-RAS-IN-1 or vehicle orally, or six i.p. injections and 4 i.v. injections. Tumor size is measured by electronic caliper every 2 d and calculated[1].

References:

[1]. Welsch ME, et al. Multivalent Small-Molecule Pan-RAS Inhibitors. Cell. 2017 Feb 23;168(5):878-889.e29.

化学性质

Cas No. 1835283-94-7 SDF
Canonical SMILES O=C(C1(N)CCNCC1)NCCCN2C3=CC=C(CN4CCN(CC5=C(Cl)C=CC=C5Cl)CC4)C=C3C(C6=CC=C(OC(F)(F)F)C=C6)=C2
分子式 C36H41Cl2F3N6O2 分子量 717.65
溶解度 DMSO : ≥ 50 mg/mL (69.67 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.3934 mL 6.9672 mL 13.9344 mL
5 mM 0.2787 mL 1.3934 mL 2.7869 mL
10 mM 0.1393 mL 0.6967 mL 1.3934 mL
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