2. TGF-beta/Smad
  3. TGF-β Receptor
  4. BMS-986260

BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively.

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BMS-986260 Chemical Structure

BMS-986260 Chemical Structure

CAS No. : 2001559-19-7

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5 mg USD 200 In-stock
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Based on 1 publication(s) in Google Scholar

BMS-986260 Related Antibodies

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Description

BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively[1].

In Vitro

BMS-986260 is a highly potent TGFβR1 inhibitor in both human (Kiapp=0.8 nM) and mouse (Kiapp= 1.4 nM) biochemical assays. BMS-986260 also inhibits TGFβ induced SMAD phosphorylation in NIH3T3 cell line, primary human T cells, and mouse and human whole blood. BMS-986260 inhibits TGF-β mediated induction of regulatory T cell (Treg) by downregulation of FOXP3 expression and a repression of CD25 with an IC50 of 230 nM[1].

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

BMS-986260 Related Antibodies
Molecular Weight

382.78

Formula

C18H12ClFN6O
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CC1=CN=C2C=CC(C3=C(C4=CC=C(F)C(Cl)=C4)N=CN3CCO)=NN21
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 : 125 mg/mL (326.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6125 mL 13.0623 mL 26.1247 mL
5 mM 0.5225 mL 2.6125 mL 5.2249 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.03%

COA (261 KB) HNMR (137 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6125 mL 13.0623 mL 26.1247 mL 65.3117 mL
5 mM 0.5225 mL 2.6125 mL 5.2249 mL 13.0623 mL
10 mM 0.2612 mL 1.3062 mL 2.6125 mL 6.5312 mL
15 mM 0.1742 mL 0.8708 mL 1.7416 mL 4.3541 mL
20 mM 0.1306 mL 0.6531 mL 1.3062 mL 3.2656 mL
25 mM 0.1045 mL 0.5225 mL 1.0450 mL 2.6125 mL
30 mM 0.0871 mL 0.4354 mL 0.8708 mL 2.1771 mL
40 mM 0.0653 mL 0.3266 mL 0.6531 mL 1.6328 mL
50 mM 0.0522 mL 0.2612 mL 0.5225 mL 1.3062 mL
60 mM 0.0435 mL 0.2177 mL 0.4354 mL 1.0885 mL
80 mM 0.0327 mL 0.1633 mL 0.3266 mL 0.8164 mL
100 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6531 mL
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BMS-986260 Related Classifications

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:

BMS-9862602001559-19-7BMS986260BMS 986260TGF-β ReceptorTransforming growth factor beta receptorsselectiveoralTGFβR1MINKNHLF cellspSMAD2/3nuclear translocationFOXP3 expressionCD25Inhibitorinhibitorinhibit

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