BMS-707035

製品コードS1366 バッチS136601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₉FN₄O₅S
	分子量	410.42	CAS No.	729607-74-3
Solubility (25°C)*	体外	DMSO	38 mg/mL (92.58 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
in vitro	BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first integrase inhibitor licensed for clinical use. This compound is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM. ^[1] However, several IN mutations, including V75I, Q148R, V151I, and G163R are found to confer resistance to HIV IN inhibitors. The binding of this compound and target DNA to IN are mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by this chemical is overcome by increasing amount of target DNA. The binding affinity of this compound to IN is also affected by the four terminal bases at the 5' end of the pre-processed U5 long terminal repeat (LTR). Gln¹⁴⁸ of IN is crucial for the binding of this chemical to IN. ^[1] The 3' terminus of the viral LTR, on the other hand, retards the rate of this compound association with IN, by regulating the kinetics of binding and dissociation. ^[2]

製品説明

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

in vitro

BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first integrase inhibitor licensed for clinical use. This compound is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM. ^[1] However, several IN mutations, including V75I, Q148R, V151I, and G163R are found to confer resistance to HIV IN inhibitors. The binding of this compound and target DNA to IN are mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by this chemical is overcome by increasing amount of target DNA. The binding affinity of this compound to IN is also affected by the four terminal bases at the 5' end of the pre-processed U5 long terminal repeat (LTR). Gln¹⁴⁸ of IN is crucial for the binding of this chemical to IN. ^[1] The 3' terminus of the viral LTR, on the other hand, retards the rate of this compound association with IN, by regulating the kinetics of binding and dissociation. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Determination of Strand Transfer Activity and Inhibition
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参考

https://pubmed.ncbi.nlm.nih.gov/17715137/
https://pubmed.ncbi.nlm.nih.gov/18991395/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Activation of PERK-ATF4-CHOP pathway as a novel therapeutic approach for efficient elimination of HTLV-1-infected cells. [ Blood Adv, 2020, 12;4(9):1845-1858]	PubMed: 32369565

Activation of PERK-ATF4-CHOP pathway as a novel therapeutic approach for efficient elimination of HTLV-1-infected cells. [ Blood Adv, 2020, 12;4(9):1845-1858]

PubMed: 32369565

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。