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BCR-ABL-IN-2

カタログ番号GC33368

BCR-ABL-IN-2 は BCR-ABL1 チロシンキナーゼの阻害剤であり、ABL1native および ABL1T315I の IC50 はそれぞれ 57 nM、773 nm です。

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BCR-ABL-IN-2 化学構造

Cas No.: 897369-18-5

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Sample solution is provided at 25 µL, 10mM.

Product Documents

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Background

BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.

BCR-ABL-IN-2 (Compound 1) contains a urea moiety to allow a hydrogen bond with the conserved K271-E286 salt bridge of ABL1, a t-butyl moiety to bind into the hydrophobic spine at the third pocket position, and a 2,3-dichlorophenyl ring to stabilize the DFG-phenylalanine F382 in the Type II-out conformation. BCR-ABL-IN-2 exhibits an IC50 of 57 nM for ABL1native and an IC50 of 773 nM for ABL1T315I[1]. Despite ABL, BCR-ABL-IN-2 can also inhibit KDR, BRaf, p38 kinase with IC50s of 1.8 μM, 0.23 μM, 6.3 nM, 43 nM, respectively[2].

[1]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011 Apr 12;19(4):556-68. [2]. ARYL SULFONOHYDRAZIDES. US 2008/0113967 A1.

Chemical Properties

Cas No. 897369-18-5 SDF
Canonical SMILES O=C([C@H]1NCC2=C(C=C(N3N=C(C(C)(C)C)C=C3NC(NC4=CC=CC(Cl)=C4Cl)=O)C=C2)C1)O
Formula C24H25Cl2N5O3 M.Wt 502.39
溶解度 Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9905 mL 9.9524 mL 19.9049 mL
5 mM 0.3981 mL 1.9905 mL 3.981 mL
10 mM 0.199 mL 0.9952 mL 1.9905 mL
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