Tofacitinib (CP-690550) Citrate
Catalog No.: GC17586Purity:>99.50%Synonyms: CP 690,550
A pan-JAK inhibitor
제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.
Cas No.: 540737-29-9
10mM (in 1mL DMSO)In Stock
$42.00
1
10mgIn Stock
$37.00
1
50mgIn Stock
$73.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $42.00 | In Stock | 1 | |
| 10mg | $37.00 | In Stock | 1 | |
| 50mg | $73.00 | In Stock | 1 |
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인용 문헌 (Citations)
1 publications이 제품을 사용한 연구자들의 논문제품 설명 (Description)
Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (Kd). The report includes additional binding for Tofacitinib at Camk1 (Kd of 5,000 nM), DCamkL3 (Kd of 4.5 nM), Mst2 (Kd of 4,300 nM), Pkn1 (Kd of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (Kd of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (Kd of 1,200 nM), Snark (Kd of 420 nM), Tnk1 (Kd of 640 nM) and Tyk2 (Kd of 620 nM)[1]. K562, KCL22, and THP-1 cells are exposed to different doses of STI571 or JAK inhibitors for 72 h to quantify the effects of tyrosine kinase inhibitor (TKI) activity. Cell growth inhibition is then evaluated using the MTT assay. The proliferation of K562 and KCL22 cells, but not THP-1 cells, is inhibited by IMA in a concentration-dependent manner. The IC50 value of IMA is 0.28 µM for K562 and 0.17 µM for KCL22. Although treatment with Tofacitinib (TOF) or INCB018424 alone does not suppress cell proliferation, both Tofacitinib and INCB018424 make the K562 and KCL22 more sensitive to IMA[4].
Animals that are treated with Tofacitinib show a significantly lower production of anti-drug antibodies (ADAs) compare with PEG-treated control mice (for five weeks after initial immunization, p4 hours[3].
References:
[1]. Jiang JK, et al. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem. 2008 Dec 25;51(24):8012-8.
[2]. Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193(1):48-55.
[3]. LaBranche TP, et al. JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production. Arthritis Rheum. 2012 Nov;64(11):3531-42.
[4]. Yagi K, et al. Pharmacological inhibition of JAK3 enhances the antitumor activity of STI571 in human chronic myeloid leukemia. Eur J Pharmacol. 2018 Apr 15;825:28-33.
실험 프로토콜 (Protocol)
| Cell experiment [1]: | |
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Cell lines |
Naïve T cell |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
16h; 50 nM |
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Applications |
A concentration of 100 nM. 50 nM, but not 10 nM, CP-690,550 suppressed IFN- c production 4 days after Th1 differentiation conditions were established, while both 10 nM and 50 nM CP-690,550 strongly suppressed IL-4 production under Th2 differentiation conditions. This suggests that CP-690,550 inhibits both Th1 and Th2 differentiation, and that Th2 is more sensitive than Th1 to this drug. We then examined the effect of CP-690,550 on Th17 and induced T regulatory (iTreg) cells. CP-690,550 enhanced IL-17 production while suppressing Foxp3 and IL-10 induction in a dose-dependent manner under Th17 differentiation conditions. These data indicate that <100 nM CP-690,550 efficiently inhibits Th1, Th2 and iTreg while promoting Th17, in vitro. |
| Animal experiment [1]: | |
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Animal models |
C57BL6/J mice and DBA/1J mice |
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Dosage form |
30 nM; intraperitoneal injection |
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Applications |
Naïve CD4+T cells isolated from mice were stimulated with various cytokines in the presence of various concentrations of CP-690,550. CP-690,550 selectively inhibited IFN c -induced STAT1, IL-4-induced STAT6, and IL-2-induced STAT5 at 3–30 nM, while 30 nM CP-690,550 did not suppress IL-6-induced STAT3 phosphorylation. A concentration greater than 100 nM was required for the partial suppression of STAT3 |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Yoshida H, Kimura A, Fukaya T, et al. Low dose CP-690,550 (tofacitinib), a pan-JAK inhibitor, accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation[J]. Biochemical and biophysical research communications, 2012, 418(2): 234-240. | |
제품 문서 (Product Documents)
Purity:>99.50%Appearance:A solid
화학적 특성 (Chemical Properties)
CAS 번호
540737-29-9
동의어
CP 690,550
화학명
2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
SMILES
CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
분자식
C16H20N6O.C6H8O7
분자량
504.49
용해도
≥ 25.22 mg/mL in DMSO, ≥ 3.4 mg/mL in Water with ultrasonic and warming
보관
4°C, protect from light
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.
계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도
g/mol
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