2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. TAK-901

TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.

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TAK-901

TAK-901 화학구조

CAS No. : 934541-31-8

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 5 publication(s) in Google Scholar

Other Forms of TAK-901:

TAK-901 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Protocol

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.

IC50 & Target[1]

Aurora A

21 nM (IC50)

Aurora B

15 nM (IC50)

In Vitro

TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A[1].
TAK-901 suppresses histone H3 phosphorylation in a dose-dependent manner with an EC50 value of 0.16 μM in PC3 cells[1].
TAK-901 is a substrate of the P-glycoprotein (PgP) drug efflux pump, as shown by the decrease in EC50 from 38 nM in the uterine sarcoma MES-SA cells to more than 50 μM in drug-resistant MES-SA/Dx5 expressing high levels of PgP[1].

Cell line EC50 (μM)
A2780 0.085
A375 0.39
A498 0.2
A549 0.13
COLO205 0.11
DLD1 1.5
H226 0.11
H358 0.077
H460 0.81
HT29 0.062
MDA-MB-435S 0.12
MES-SA 0.043
MKN-45 0.16
PC3 0.19
IMR-90 0.088

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

TAK-901 Related Antibodies
In Vivo

TAK-901 (In A2780 and AML MV4-11 nude mice xenograft model) causeS tumor stasis for 30 days at 30 and 40 mg/kg/injection, respectively[1].

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

504.64

화학식

C28H32N4O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1CCN(CC1)C)C2=C(C3=C(C4=CC(C)=CN=C4N3)C(C5=CC=CC(S(=O)(CC)=O)=C5)=C2)C
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : 65 mg/mL (128.80 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 1.9816 mL 9.9081 mL 19.8161 mL
5 mM 0.3963 mL 1.9816 mL 3.9632 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
순도&문서

Purity: 99.84%

SDS (393 KB)

COA (256 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Enzyme activities of Aurora A/TPX2 and Aurora B/INCENP complexes are assayed at room temperature in buffer containing serially diluted TAK-901, and the product is quantified using IMAP detection reagents. Aurora A/TPX2 (2 nM) is assayed with 100 nM FL-Kemptide and 1 mM ATP. Aurora B/INCENP (0.8 nM) is assayed with 100 nM 5-carboxy-fluorescein-GRTGRRNSI-NH2 (FL-PKAtide) and 10 mM ATP. For time-dependent inhibition, Aurora B/INCENP is incubated with TAK-901 for 1 hour at room temperature followed by addition of 150 mM ATP to initiate the reaction[1].

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Cell Assay 
[1]

Cells are plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation is determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA. IMR-90 immortalized lung fibroblasts are seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells are then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay is conducted[1].

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration
[1]

Mice: Tumor-bearing mice or rats are treated intravenously twice daily (b.i.d.) with either vehicle or TAK-901 on 2 consecutive days per week or every other day for 2 or 3 cycles. The antitumor activity of TAK-901 in human tumor and leukemia xenograft models are monitored[1].

Nude rats bearing A2780 tumors averaging 250 to 500 mg receive an intravenous dose of TAK-901. Plasma samples are collected by terminal cardiac puncture under CO2 anesthesia. Tumors are dissected and snap-frozen at -80°C[1].

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9816 mL 9.9081 mL 19.8161 mL 49.5403 mL
5 mM 0.3963 mL 1.9816 mL 3.9632 mL 9.9081 mL
10 mM 0.1982 mL 0.9908 mL 1.9816 mL 4.9540 mL
15 mM 0.1321 mL 0.6605 mL 1.3211 mL 3.3027 mL
20 mM 0.0991 mL 0.4954 mL 0.9908 mL 2.4770 mL
25 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9816 mL
30 mM 0.0661 mL 0.3303 mL 0.6605 mL 1.6513 mL
40 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2385 mL
50 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
60 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 mL
80 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6193 mL
100 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4954 mL
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TAK-901 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:

TAK-901934541-31-8TAK901TAK 901Aurora KinaseInhibitorinhibitorinhibit

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상품명:
TAK-901
Cat. No.:
HY-12201
수량:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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