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  4. TBC3486

TBC3486 is a highly selective integrin α4β1 inhibitor. TBC3486 acts as a chemosensitizer to enhance the sensitivity of leukemia cells to chemotherapy. TBC3486 exhibits efficacy in preclinical models of integrin α4-dependent inflammatory and autoimmune diseases, including a mouse model of autoimmune encephalomyelitis. TBC3486 can be used for the research of precursor B-cell acute lymphoblastic leukemia.

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TBC3486

TBC3486 Chemical Structure

CAS No. : 247044-77-5

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TBC3486 Related Antibodies

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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Description

TBC3486 is a highly selective integrin α4β1 inhibitor. TBC3486 acts as a chemosensitizer to enhance the sensitivity of leukemia cells to chemotherapy. TBC3486 exhibits efficacy in preclinical models of integrin α4-dependent inflammatory and autoimmune diseases, including a mouse model of autoimmune encephalomyelitis. TBC3486 can be used for the research of precursor B-cell acute lymphoblastic leukemia[1].

In Vitro

TBC3486 (5-25 μM; 4 days) dose-dependently reduces adhesion of pre-B-ALL LAX7R cells to OP9 stromal cells[1].
TBC3486 (25 μM; 4 days) specifically downregulates integrin α4 expression in pre-B-ALL LAX7R cells without altering integrin α5 or integrin α6 expression[1].
TBC3486 (25 μM; 2 days) significantly reduces adhesion of pre-B-ALL LAX7R, ICN3, and SFO3 cells to human VCAM-1, with the greatest effect observed in CD49d-high LAX7R cells[1].
TBC3486 (25 μM; 2 days) does not affect the viability of pre-B-ALL LAX7R, ICN3, or SFO3 cells[1].
TBC3486 (25 μM; 4 days, in combination with VDL chemotherapy) sensitizes pre-B-ALL LAX7R, ICN3, and SFO3 cells to Vincristine (HY-N0488A), Dexamethasone (HY-14648) and L-asparaginase (HY-P1923) chemotherapy, significantly reducing cell viability compared to chemotherapy alone[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TBC3486 Related Antibodies

Cell Viability Assay[1]

Cell Line: Patient-derived pre-B-cell acute lymphoblastic leukemia (pre-B-ALL) LAX7R, ICN3, and SFO3 cells
Concentration: 25 μM
Incubation Time: 2 days
Result: Had no effect on the viability of LAX7R, ICN3, or SFO3 cells compared to control.
In Vivo

TBC3486 (10 mg/kg/day; i.p.; two injections per day; daily for 2 weeks) prolongs survival of NOD/SCID mice bearing human LAX7R pre-B-ALL xenografts, with a median survival time of 41 days as monotherapy and 82 days when combined with VDL chemotherapy[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID (xenotolerant)[1]
Dosage: 10 mg/kg/day
Administration: i.p.; two injections per day; daily for 2 weeks
Result: Extended median survival time to 41 days compared to control MST of 33 days.
Molecular Weight

557.68

Formula

C27H31N3O6S2
CAS No.
SMILES

[C@H](NC(N[C@H](C(N(CC1=CC=CS1)CC2=CC=CS2)=O)CCCC)=O)(CC(O)=O)C=3C=C4C(=CC3)OCO4
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TBC3486 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TBC3486247044-77-5TBC 3486TBC-3486IntegrinVDL chemotherapypre-B-cell acute lymphoblastic leukemiaautoimmune encephalomyelitisMIDAS siteVCAM-1pre-B-ALL cellsintegrin α4β7OP9 stromal cellsintegrin α4β1pre-B-ALL xenograftsInhibitorinhibitorinhibit

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