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BMS986260

SKU: orb1298679

Description

BMS986260

Research Area

Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number2001559-19-7
MW382.78
Purity97.67%
FormulaC18H12ClFN6O
SMILESC(CO)N1C(=C(N=C1)C2=CC(Cl)=C(F)C=C2)C3=NN4C(C=C3)=NC=C4C#N
TargetTGF-beta/Smad
SolubilityDMSO:25 mg/mL (65.31 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (5.22 mM)

Bioactivity

In Vitro
BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models. Since daily dosing of TGFβR1 inhibitors is known to cause class-based cardiovascular (CV) toxicities in preclinical species, a dosing holiday schedule in the anti-PD-1 combination efficacy studies was explored. An intermittent dosing regimen of 3 days on and 4 days off allowed mitigation of CV toxicities in one month dog and rat toxicology studies and also provided similar efficacy as once daily dosing.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

BMS 986260, BMS986260, BMS-986260, CD25, FOXP3 expression, Inhibitor, NHLF cells, nuclear translocation, oral, MINK, inhibit, selective, pSMAD2/3, Smad, TGF-b/Smad, TGFbeta, TGFb, TGFbeta/Smad, TGF-beta, TGF-β/Smad, TGF-β Receptor, TGFβ, Transforming growth factor beta receptors, TGFβR1

Similar Products

  • BMS986260 [orb1219569]

    >98% (HPLC)

    2001559-19-7

    382.07

    C18H12ClFN6O

    1 g, 500 mg, 200 mg, 5 mg, 10 mg, 50 mg, 25 mg, 100 mg
Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

BMS986260 (orb1298679)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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1 mg
$ 120.00
1 ml x 10 mM (in DMSO)
$ 180.00
5 mg
$ 210.00
10 mg
$ 290.00
25 mg
$ 440.00
50 mg
$ 640.00
100 mg
$ 890.00
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