1. Epigenetics
  2. Histone Methyltransferase
  3. MLL1-IN-1

MLL1-IN-1 is an orally active MLL1 inhibitor with an IC50 of 0.043 μM. MLL1-IN-1 induces Menin protein degradation and inhibits the proliferation of leukemia cells. MLL1-IN-1 can induce tumor regression in leukemia-bearing mice. MLL1-IN-1 is useful for research into MLL1-associated leukemia.

For research use only. We do not sell to patients.

MLL1-IN-1

MLL1-IN-1 Chemical Structure

CAS No. : 3058433-50-1

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Description

MLL1-IN-1 is an orally active MLL1 inhibitor with an IC50 of 0.043 μM. MLL1-IN-1 induces Menin protein degradation and inhibits the proliferation of leukemia cells. MLL1-IN-1 can induce tumor regression in leukemia-bearing mice. MLL1-IN-1 is useful for research into MLL1-associated leukemia[1].

In Vitro

MLL1-IN-1 (7 days) inhibits the viability of MOLM-13, MV-4-11, and OCI-AML3 cells, with IC50 values ​​of 0.04, 0.035, and 0.047 μM, respectively[1].

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

In Vivo

MLL1-IN-1 (30-200 mg/kg, p.o., twice daily for 14 days) induces tumor regression in an MV-4-11 subcutaneous xenograft mouse model[1].
MLL1-IN-1 (30-200 mg/kg, p.o., once daily for 21/90 days) induces tumor regression in a MOLM-13 subcutaneous xenograft mouse model[1].
MLL1-IN-1 (150 mg/kg, p.o., once daily for 21 days) prolongs survival in an MLL-r AML patient-derived xenograft (PDX) mouse model[1].

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

Animal Model: Female CB17 SCID mice with MV-4-11 subcutaneous xenograft[1]
Dosage: 30, 100, 200 mg/kg
Administration: p.o., twice daily for 14 days
Result: Reduced tumors by 88%, with a 100% recurrence rate following drug discontinuation at a dose of 30 mg/kg. Reduced tumors by 97%/99%, with no recurrence observed 6 weeks after drug discontinuation at doses of 100/200 mg/kg.
Molecular Weight

589.74

Formula

C34H44FN5O3

CAS No.
SMILES

FC1=CC=[C@]([N@]2C(C=NC=C3)=C3C(C(C4CCN(C([C@@H]5CCC(C)(C)N5)=O)CC4)=O)=C2C)C(C(N(C(C)C)C(C)C)=O)=C1

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  • 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.

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Product Name:
MLL1-IN-1
Cat. No.:
HY-182793
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