2. Neuronal Signaling
    Stem Cell/Wnt
  3. γ-secretase
    Notch
  4. BMS-906024

BMS-906024 

Cat. No.: HY-15670 Purity: 98.10%
COA Handling Instructions

BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.

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

BMS-906024 Chemical Structure

BMS-906024 Chemical Structure

CAS No. : 1401066-79-2

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10 mg USD 2400 In-stock
25 mg USD 5200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BMS-906024

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  • Purity & Documentation

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  • Customer Review

Description

BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity[1][2].

IC50 & Target

IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)[2]
In Vitro

BMS-906024 (5-100 nM; 72 hours) reduces Notch1 ICD levels in all six lung cancer cell lines. BMS-906024 at 100 nM, has no effect on total Notch1, and down-regulated Hes1 transcript[1].
In cancer cell proliferation assays, BMS-906024 inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of ∼4 nM[2].
BMS-906024 (100 nM; for 72 hours) enhances the anti-tumor activity of Paclitaxel in vitro[1].

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

Western Blot Analysis[1]

Cell Line: NSCLC cell lines (A549, H358, H1975, H2444, H1792, HCC44)
Concentration: 5, 10, 25, 50, 100 nM
Incubation Time: 72 hours
Result: Reduced Notch1 ICD levels in all six lung cancer cell lines tested at concentrations as low as 5 nM, with maximal depletion at 50-100 nM.
In Vivo

BMS-906024 (8.5 mg/kg; oral gavage; days 1 through 4 of each week for 3 weeks) significantly enhances the tumor growth inhibition of Paclitaxel (36 mg/kg). BMS-906024 enhances Paclitaxel-mediated cytotoxicity in vivo in NSCLC through a combination of inhibiting proliferation and promoting apoptosis, in a p21 and p57-independent manner[1].
BMS-906024 has a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO[2].

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

Animal Model: Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenografts[1]
Dosage: 8.5 mg/kg
Administration: oral gavage; days 1 through 4 of each week for 3 weeks
Result: Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment.
Animal Model: Mouse[2]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO.
Clinical Trial
Molecular Weight

556.50

Appearance

Solid

Formula

C26H26F6N4O3
CAS No.
SMILES

O=C(N[[email protected]@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[[email protected]](CCC(F)(F)F)[[email protected]](CCC(F)(F)F)C(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 9.5 mg/mL (17.07 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7969 mL 8.9847 mL 17.9695 mL
5 mM 0.3594 mL 1.7969 mL 3.5939 mL
10 mM 0.1797 mL 0.8985 mL 1.7969 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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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.

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Keywords:

BMS-9060241401066-79-2BMS906024BMS 906024γ-secretaseNotchGamma secretaseoralNotch1Notch2Notch3Notch4broad-spectrumantineoplasticInhibitorinhibitorinhibit

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