成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

  2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. FLT3 CDK
  4. AMG 925

AMG 925 是一種有效的選擇性的 FLT3/CDK4 雙重抑制劑，IC50 分別為 2±1 nM 和 3±1 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

我們將采用定制合成服務(wù)的方式為您快速提供所需產(chǎn)品和技術(shù)服務(wù)

AMG 925 Chemical Structure

AMG 925 Chemical Structure

CAS No. : 1401033-86-0

1.  客戶無(wú)需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥323
In-stock
5 mg ￥850
In-stock
10 mg ￥1200
In-stock
25 mg ￥2200
In-stock
50 mg ￥3500
In-stock
100 mg ￥5288
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of AMG 925:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.

IC50 & Target[1]

FLT3

2 nM (IC50)

CDK4

3 nM (IC50)

CDK6

8 nM (IC50)

CDK2

375 nM (IC50)

CDK1

1.9 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
COLO 205 IC50
0.055 μM
Compound: 28, AMG 925
Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
[PMID: 24641103]
MDA-MB-436 IC50
3.83 μM
Compound: 28, AMG 925
Antiproliferative activity against Rb-negative human MDA-MB-436 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
Antiproliferative activity against Rb-negative human MDA-MB-436 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
[PMID: 24641103]
MOLM-13 IC50
0.005 μM
Compound: 28, AMG 925
Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs
Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs
[PMID: 24641103]
MOLM-13 IC50
0.019 μM
Compound: 28, AMG 925
Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
[PMID: 24641103]
MOLM-13 IC50
0.023 μM
Compound: 28, AMG 925
Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs
Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs
[PMID: 24641103]
MOLM-13 IC50
0.023 μM
Compound: 28, AMG 925
Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
[PMID: 24641103]
MOLM-13 IC50
0.028 μM
Compound: 28, AMG 925
Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 4 months by beta-plate counting analysis
Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 4 months by beta-plate counting analysis
[PMID: 24641103]
MOLM-13 ED50
22 mg/kg
Compound: 28, AMG 925
Antitumor activity against human MOLM13 cells xenografted in po dosed CrTac:NCR-Foxn1nu (NCR) nude mouse assessed as tumor growth inhibition administered qd for 8 days
Antitumor activity against human MOLM13 cells xenografted in po dosed CrTac:NCR-Foxn1nu (NCR) nude mouse assessed as tumor growth inhibition administered qd for 8 days
[PMID: 24641103]
U-937 IC50
0.052 μM
Compound: 28, AMG 925
Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
[PMID: 24641103]
體外研究
(In Vitro)

AMG 925 also inhibits CDK6, CDK2, and CDK1 in kinase assays with IC50s of 8±2 nM, 375±150 nM, 1.90±0.51 μM, respectively. A fair overall kinase selectivity of AMG 925 is as determined by KinomScan against a panel of 442 various kinases. Cellular selectivity (on-target vs. off-target activity) of AMG 925 is about 50-fold as evaluated by comparison of its growth-inhibiting activity in RB-positive (RB+) and RB-negative (RB-) non- acute myeloid leukemia (AML) cancer cell lines. AMG 925 potently inhibits growth of AML cell lines MOLM13 (FLT3-ITD; IC50=19 μM) and Mv4-11 (FLT3-ITD; IC50=18 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

MOLM13 tumor-bearing mice are dosed twice daily by oral administration 6 hours apart with 12.5, 25, or 37.5 mg/kg AMG 925. Tumors are then harvested 3, 9, 12, and 24 hours after the first dose, and analyzed for levels of P-STAT5 and P-RB. Maximum inhibition of P-STAT5 and P-RB is achieved at 6 and 12 hours respectively at the 37.5 mg/kg dose of AMG 925. Interestingly, a rebound of P-STAT5 at 24 hours is observed, possibly as a result of compensational feedback. The pharmacodynamic responses of P-STAT5 and P-RB inhibition correlated with plasma concentrations of AMG 925. AMG 925 inhibits AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlates with the inhibition of STAT5 and retinoblastoma protein (RB) phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 is also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and Sorafenib)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

471.55

Formula

C26H29N7O2
CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Cell Assay
[1]

MOLM13 and Mv4-11 are used. MOLM13-Luc cells are constructed by transduction of MOLM13 cells with the pLV218G luciferin/lentivector, which expresses luciferase under the murine EF1α promoter. Sorafenib-resistant MOLM13 (MOLM13sr) and Mv4-11 (Mv4-11sr) are isolated by passaging the cells in growth medium containing increasing concentrations of Sorafenib (1-1 nM). Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5×103 cells/well in a total volume of 160 μL. Test compounds (e.g., AMG 925; 0.03 and 0.3μM) are serially diluted into the plate (20 μL/well) and 20 μL/0.1 μCi of [14C]-Thymidine added to each well. Isotope incorporation is determined using a β plate counter after further 72-hour incubation. Apoptosis is assayed by using the Vybrant Apoptosis Assay Kit. Briefly, cells are seeded into a 6-well plate at 5×105 cells per well and treated with compounds (e.g., AMG 925; 0.003, 0.01, 0.03, 0.1, 0.3, and 1 μM) for 24 hours. The cells are then stained with reagents provided in the kit and analyzed by flow cytometry. The Sytox Green fluorescence versus allophycocyanin fluorescence dot plot shows resolution of live, apoptotic, and dead cells, which are quantified using the Flowjo software. The cell-cycle analysis is done by treating the cells with AMG 925 for 24 hours followed by using the CycleTest Kit. Ten thousand events are acquired and the proportions of cells in each cycle phase are calculated using the ModFit software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
CrTac:NCR-Foxn1nu (NCR) nude mice are used. 2×106 cells are innoculated on the flank of NCR nude mice and allowed to grow for 13 days. Mice are then dosed twice a day by oral administration 6 hours apart with 12.5, 25, 37.5, and 50 mg/kg of AMG 925 for 10 consecutive days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)
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.

您最近查看的產(chǎn)品:

Your information is safe with us. * Required Fields.

   產(chǎn)品名稱：

  

* 需求量：

* 客戶姓名：

 

* Email：

* 電話：

 

* 公司或機(jī)構(gòu)名稱：

   留言給我們：

Bulk Inquiry

Inquiry Information

產(chǎn)品名稱：
AMG 925
目錄號(hào)：
HY-15889
需求量：