2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. BMS-986365

BMS-986365  (Synonyms: CC-94676)

製品番号: HY-158101 純度: 99.92%
COA 取扱説明書 Technical Support

BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC).
(Pink: Androgen Receptor ligand (HY-168697); Blue: Cereblon ligand (HY-W247437); Black: linker).

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BMS-986365

BMS-986365 構造式

CAS 番号 : 2446928-30-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 351 在庫あり
Solution
10 mM * 1 mL in DMSO USD 351 在庫あり
Solid
5 mg $195 在庫あり
10 mg $305 在庫あり
25 mg $495 在庫あり
50 mg $690 在庫あり
100 mg $970 在庫あり
250 mg $1500 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

BMS-986365 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC)[1][2][3][4]. (Pink: Androgen Receptor ligand (HY-168697); Blue: Cereblon ligand (HY-W247437); Black: linker).

体外実験

BMS-986365 (0.05-5 μM; 6 h) maintains low levels of AR protein despite increased AR transcript levels in VCaP and LNCaP cells[3].
BMS986365 (0.1-10 μM; 6-72 hours) inhibits AR target gene transcription and AR-dependent proliferation in VCaP and LNCaP cells[3].
BMS-986365 exhibits AR degradation potency in VCaP (ARWT amplified) cells with a GI50: 753 nM)[3].
BMS-986365 shows a difference in degradation potency in VCaP cells and LNCaP cells, with DC50 values of 7 nM and 29 nM, respectively[3].
BMS986365 potently inhibits androgen-stimulated proliferation of VCaP and LNCaP cells but showed little antiproliferative effect in 22Rv1 or PC3 cells[3].
BMS986365 inhibits R1881-stimulated proliferation of VCaP and LNCaP cells with GI50 values of 11 and 4 nM, respectively[3].

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

BMS-986365 関連抗体

Western Blot Analysis[3]

Cell Line: VCaP and LNCaP cells
Concentration: 0.05 μM, 0.5 μM, and 5 μM
Incubation Time: 6 h
Result: Indicated strong degradation of AR.
The T1/2 for AR degradation at 500 nM was ~0.6 and ~1.3 hours for VCaP and LNCaP cells, respectively.

RT-PCR[3]

Cell Line: VCaP and LNCaP cellsVCaP and LNCaP cells treated with R1881
Concentration: 0.1 μM, 1 μM, or 10 μM
Incubation Time: 6, 24, or 72 hours
Result: Exerted a potent inhibitory effect on androgen upregulated FKBP5 expression, with IC50 values of 1 and 4 nM for VCaP and LNCaP, respectively.
Parmacokinetics
Species Dose Route Cmax Tmax F CLblood Vd T1/2
Mice[3] 10 mg/kg p.o. 0.275 μM 4.5 h 40 % / / /
Mice[3] 2 mg/kg i.v. / / / 20.7 mL/min/kg 3.1 L/kg 1.7 h
体内実験

BMS986365 (30 mg/kg; p.o.; once daily; for 3 consecutive days) demonstrates on-target activity, degrading AR, suppressing AR signaling in VCaP or HR-VCaP tumors propagated in intact NSG male mice[3].
BMS-986365 (p.o.; for 7 days once daily) shows dose-dependent degradation of AR in male beagle dogs and sexually immature cynomolgus monkeys[3].
BMS986365 (30 mg/kg; p.o.; once daily; for 45 consecutive days) exhibits significant antitumor activity in a VCaP mouse xenograft model[3].

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

Animal Model: Male 6- to 8-week-old intact or castrated NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) were inoculated with 5 x 106 VCaP or HR-VCaP cells[3]
Dosage: 30 mg/kg
Administration: p.o.; once daily; for 3 consecutive days
Result: Evaluation of plasma and tumor samples indicated good compound exposure in both the circulation and within tumors at 2, 6, and 24 hours after the last dose.
Reduced AR to 91% and 83% of control levels at 6 and 24 hours, respectively, after the last dose.
Animal Model: Male NSG mice were inoculated with 5 x 106 HR-VCaP tumor cells into the right flank[3].
Dosage: 30 mg/kg
Administration: p.o.; once daily for 45 consecutive days.
Result: Exhibited significant antitumor activity in a VCaP xenograft model, exhibiting 81% tumor volume reduction in intact mice.
臨床実験
分子量

818.91

分子式

C41H45F3N8O5S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C(F)(F)F)C=C(N2C(N(C3=CC=C(OCCN4C[C@@H](C)N(CC(NC5=CC=CC(NC6C(NC(CC6)=O)=O)=C5)=O)CC4)C(CC)=C3)C(C)(C)C2=O)=S)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (122.11 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 1.2211 mL 6.1057 mL 12.2114 mL
5 mM 0.2442 mL 1.2211 mL 2.4423 mL
10 mM 0.1221 mL 0.6106 mL 1.2211 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3.75 mg/mL (4.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.92%

COA (244 KB) HNMR (558 KB) LCMS (92 KB)

取扱説明書 (2659 KB)
参考文献

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 1.2211 mL 6.1057 mL 12.2114 mL 30.5284 mL
5 mM 0.2442 mL 1.2211 mL 2.4423 mL 6.1057 mL
10 mM 0.1221 mL 0.6106 mL 1.2211 mL 3.0528 mL
15 mM 0.0814 mL 0.4070 mL 0.8141 mL 2.0352 mL
20 mM 0.0611 mL 0.3053 mL 0.6106 mL 1.5264 mL
25 mM 0.0488 mL 0.2442 mL 0.4885 mL 1.2211 mL
30 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0176 mL
40 mM 0.0305 mL 0.1526 mL 0.3053 mL 0.7632 mL
50 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.6106 mL
60 mM 0.0204 mL 0.1018 mL 0.2035 mL 0.5088 mL
80 mM 0.0153 mL 0.0763 mL 0.1526 mL 0.3816 mL
100 mM 0.0122 mL 0.0611 mL 0.1221 mL 0.3053 mL
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BMS-986365 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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-9863652446928-30-7CC-94676BMS986365BMS 986365CC94676CC 94676PROTACsAndrogen ReceptorHeterobifunctional ligand-directed degraderLDDin advanced prostate cancerInhibitorinhibitorinhibit

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