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抑制剂/激活剂

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凋亡与自噬

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Cobimetinib (GDC-0973)

Cobimetinib (GDC-0973) 考比替尼; GDC-0973; XL518

Cobimetinib (GDC-0973, RG7420)是一种有效的高选择性MEK1抑制剂，IC50 为 4.2 nM，且对其他很多丝氨酸-苏氨酸和酪氨酸激酶没有显著抑制作用。Cobimetinib 可诱导凋亡。Phase 3。

货号：
TK0379
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	934660-93-2
生物活性	Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
分子式	C22H24F3N3O2
分子量	531.31
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 100 mg/mL (188.21 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
体内研究	In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM h, respectively. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375).
体外研究	The EC50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941). Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells.
文献	•Nat Nanotechnol. 2021 Jul;16(7):830-839. •Sci Transl Med. 2021 Jan 27;13(578):eaba7308. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Bioact Mater. 8 September 2021. •Cancer Res. 2021 Feb 15;canres.2370.2020. •EMBO Mol Med. 2021 Nov 15;e14511. •Blood Cancer J. 2022 Jan 11;12(1):5. •Neuro Oncol. 2019 Mar 18;21(4):486-497. •J Control Release. 2015 Oct 21;220(Pt A):160-168. •Cell Syst. 2020 Nov 18;11(5):478-494.e9. •J Invest Dermatol. 2021 Sep 14;S0022-202X(21)01672-9. •Sci Signal. 2018 Oct 30;11(554):eaar6795. •Elife. 2021 Oct 27;10:e65759. •Cancers. 2019 Feb 1;11(2):164. •Mol Cancer Res. 2018 Mar;16(3):543-553. •Int J Oncol. 2020 Jun;56(6):1429-1441. •Biomolecules. 2021 Mar 30;11(4):518. •Exp Cell Res. 2020 Aug 1;393(1):112054. •ACS Comb Sci. 2019 Dec 9;21(12):805-816. •Oncotarget. 2020 Nov 3;11(44):3921-3932. •SSRN. 2020 May. •bioRxiv. 2019 Sep. •Methods Mol Biol. 2018;1711:351-398. •Patent. US20170326205A1. •Patent. US9724393B2. •Department of Microbiology. Oslo University. 2017 May. •Patent. US20170020964A1. •School of Health Sciences. Northeastern University. 2016 Jan.
纯度及产品资料	98%

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