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Asciminib

Catalog No. T5177 CAS 1492952-76-7

Synonyms: ABL001

Asciminib (ABL001) (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).

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Asciminib, CAS 1492952-76-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 57.00
2 mg	In stock	$ 84.00
5 mg	In stock	$ 129.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 322.00
50 mg	In stock	$ 450.00
100 mg	In stock	$ 663.00
500 mg	In stock	$ 1,390.00
1 mL * 10 mM (in DMSO)	In stock	$ 142.00

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Purity: 99.45%

Purity: 99.15%

Purity: 97.93%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Asciminib (ABL001) (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).
Targets&IC50	Abl-1:0.45 nM
In vitro	In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, ABL001 had an anti-proliferative IC50 value of 0.25nM. By contrast, the addition of IL-3 to bypass BCR–ABL1 dependence renders these cells insensitive to ABL001. In the CML blast-phase cell line KCL-22, ABL001 inhibited phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1h using concentrations that correlate with those required for inhibition of cell proliferation [1]. K562-Dox and K562-ABCG2 cells demonstrated increased LD50 (asciminib) vs K562 control cells: 256 and 299 nM respectively vs 24 nM. Sensitivity was completely restored with specific inhibitors cyclosporine (ABCB1) and Ko143 (ABCG2): K562-Dox LD50 (asciminib+cyclosporine) = 13 nM, K562-ABCG2 LD50 (asciminib+Ko143) = 15 nM [2].
In vivo	Single doses of 7.5, 15 and 30mg kg?1 ABL001, administered to mice bearing KCL22 xenografts, inhibited pSTAT5 (Tyr694), which returned to baseline at 10, 12 and 16–20h after administration of the dose, respectively. In mice implanted with KCL-22 tumours, the minimum dose of ABL001 required for complete regression was 7.5mg/kg twice a day (BID) or 30mg/kg once a day (QD), and was tolerated at doses up to 250mg kg?1 BID. Similarly, in xenografts derived from patients with Ph+ ALL, treatment with 7.5 and 30mg/kg ABL001 led to regressions that were maintained during dosing [1].
Cell Research	Cells were resuspended in fresh culture media before culture in 24-well plates in the presence of TKI or asciminib at a density of 2 × 105 cells/mL. Plates were seeded with 1 mL of cell suspension and incubated for 72 h before cell viability determination with 7-aminoactinomycin (7-AAD) and Phycoerythrin (PE)-conjugated Annexin V. Flow cytometric analysis was conducted with a BD LSRFortessa X-20 and FACSDiva software. The lethal dose of asciminib (LD50 asciminib), imatinib (LD50 IM), nilotinib (LD50 NIL) and dasatinib (LD50 DAS) required to cause 50% death of cells was calculated [2].
Animal Research	Asciminib efficacy in three patient-derived ALL systemic xenograft models (ALL-7015, AL-7119 and AL-7155) is assessed by FACS monitoring of the percentage of CD45+ cells per live cell in blood samples taken at varying time points after dosing with either 7.5 mg/kg BID (group 2) or 30 mg/kg BID (group 3) asciminib for 3 weeks [1].

Synonyms	ABL001
Molecular Weight	449.84
Formula	C20H18ClF2N5O3
CAS No.	1492952-76-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 50 mg/mL

References and Literature

1. Wylie AA, et al. The allosteric inhibitor ABL2001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737. 2. Eadie LN, et al. The new allosteric inhibitor asciminib is susceptible to resistance mediated by ABCB1 and ABCG2 overexpression in vitro. Oncotarget. 2018 Feb 3;9(17):13423-13437.

Citations

1. Zhang C, Huang C, Xia H, et al. Autophagic sequestration of SQSTM1 disrupts the aggresome formation of ubiquitinated proteins during proteasome inhibition. Cell Death & Disease. 2022, 13(7): 1-15 2. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Bioactive Compounds Library Max FDA-Approved Kinase Inhibitor Library

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Cenisertib AEE788 Vamotinib PD180970 AN-019 GNF-7 Gypsogenin Ponatinib

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Keywords

Asciminib 1492952-76-7 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl ABL-001 inhibit ABL 001 ABL001 Inhibitor inhibitor

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