Name: RMC-9805
Brand: TargetMol
SKU: T78212
Price: 883 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 883

现货

5 mg

¥ 2,330

现货

10 mg

¥ 3,400

现货

25 mg

¥ 5,560

现货

50 mg

¥ 8,110

现货

100 mg

¥ 11,970

现货

1 mL x 10 mM (in DMSO)

¥ 5,910

现货

产品介绍

生物活性

产品描述	RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
靶点活性	pERK (AsPC-1 cells):23 nM (EC50), pERK (HPAC cells):7 nM (EC50), pERK (HPAC cells):7 nM
体外活性	方法：eCT26 (KRASG12D/G12D) 和 KPCY 6499c4 (KRASG12D/+) 细胞用 RMC-9805 (100 nM) 处理 48 h，通过细胞因子阵列测量细胞因子水平，通过流式细胞术检测细胞表面表达。结果：eCT26 (KRASG12D/G12D) 和 KPCY 6499c4 (KRASG12D/+) 细胞中的 CXCL1、GM-CSF 减少，PD-L1、PVR 减少；CXCL10、CCL17 增加，MHC-Ⅰ、MHC-Ⅱ 增加。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 RMC-9805 (100 mg/kg) 口服给药给 eCT26 (KRASG12D/G12D) 异种移植瘤小鼠，每天一次，给药 4-8 天。结果：RMC-9805 在 KRAS G12D 异种移植模型中具有抗肿瘤活性。[2]
别名	Zoldonrasib, KRAS G12D inhibitor 18, KRAS G12D IN 18

化学信息

分子量	1168.44
分子式	C₆₃H₈₈F₃N₁₁O₇
CAS No.	2922732-54-3
Smiles	C(C(F)(F)F)N1C(=C2C=3C1=CC=C(C3)N4C[C@](C[C@H](NC([C@@H](N5C[C@@]6(CC5)CN(C(=O)[C@H]7[C@H](N7C)[C@@H]8CC8)CC6)[C@H]9CCCC9)=O)C(=O)N%10N[C@](C(=O)OCC(C)(C)C2)(CCC%10)[H])(OCC4)[H])C%11=C([C@@H](OC)C)N=CC(=C%11)N%12CCN(CC%12)C%13CC%13
颜色	White
物理性状	Solid

储存&溶解度

存储

keep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 252.5 mg/mL (216.1 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (4.28 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8558 mL	4.2792 mL	8.5584 mL	42.7921 mL
5 mM	0.1712 mL	0.8558 mL	1.7117 mL	8.5584 mL
10 mM	0.0856 mL	0.4279 mL	0.8558 mL	4.2792 mL
20 mM	0.0428 mL	0.2140 mL	0.4279 mL	2.1396 mL
50 mM	0.0171 mL	0.0856 mL	0.1712 mL	0.8558 mL
100 mM	0.0086 mL	0.0428 mL	0.0856 mL	0.4279 mL

体内实验配液计算器