Evofosfamide (TH-302)

目錄號：S2757 Purity: 99.82%

Evofosfamide (TH-302)是一種選擇性低氧激活的前體藥物，靶向作用于實(shí)體瘤的hypoxic區(qū)域，IC50為19 nM，在缺氧條件下比在有氧條件下細(xì)胞毒性增強(qiáng)270倍，細(xì)胞色素P450代謝穩(wěn)定。

Evofosfamide (TH-302) Chemical Structure

CAS: 918633-87-1

規(guī)格	價格	庫存
10mM (1mL in DMSO)	2612.61	現(xiàn)貨
10mg	3028.64	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.82%

99.82

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相關(guān)化合物庫	FDA藥物庫天然產(chǎn)物庫已知活性藥物庫-I 生物活性庫Ⅱ 多樣性化合物母核庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時間	活性描述	文獻(xiàn)信息
H460	Cytotoxicity assay	2 hrs	Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by clonogenic assay, IC90=0.1μM.	18257544
H460	Cytotoxicity assay	2 hrs	Cytotoxicity against human H460 cells under hypoxic condition after 2 hrs by Alamar blue staining assay, IC50=0.019μM.	18257544
HT29	Cytotoxicity assay	2 hrs	Cytotoxicity against human HT29 cells under hypoxic condition after 2 hrs by clonogenic assay, IC90=0.2μM.	18257544
H460	Cytotoxicity assay	2 hrs	Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by Alamar blue staining assay, IC50=5.1μM.	18257544
H460	Cytotoxicity assay	2 hrs	Cytotoxicity against human H460 cells under normoxic condition after 2 hrs by clonogenic assay, IC90=30μM.	18257544
HT29	Cytotoxicity assay	2 hrs	Cytotoxicity against human HT29 cells under normoxic condition after 2 hrs by clonogenic assay, IC90=40μM.	18257544
NCI-H460	Cytotoxicity assay	24 hrs	Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50=9.08μM.	28350997
HT-29	Cytotoxicity assay	24 hrs	Cytotoxicity against human HT-29 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50=49.51μM.	28350997
NCI-H460	Cytotoxicity assay	24 hrs	Cytotoxicity against human NCI-H460 cells after 24 hrs under hypoxic condition by luminescence-based Cell-Titer Glo assay, IC50=0.0093μM.	29079474
NCI-H460	Cytotoxicity assay	24 hrs	Cytotoxicity against human NCI-H460 cells after 24 hrs under normoxic condition by luminescence-based Cell-Titer Glo assay, IC50=6.65μM.	29079474
DU145	Cytotoxicity assay	2 hrs	Cytotoxicity against human DU145 cells incubated for 2 hrs under hypoxic condition measured after 72 hrs by Alamar blue assay, IC50=4.14μM.	29259746
PC3	Cytotoxicity assay	2 hrs	Cytotoxicity against human PC3 cells incubated for 2 hrs under hypoxic condition measured after 72 hrs by Alamar blue assay, IC50=6.49μM.	29259746
HEMC-SS	Antiproliferative assay	24 hrs	Antiproliferative activity against human HEMC-SS cells treated for 24 hrs under hypoxic condition followed by compound wash-out and incubated under normoxic condition for 48 hrs by alamar blue assay, IC50=0.13μM.	30199705
HEMC-SS	Antiproliferative assay	24 hrs	Antiproliferative activity against human HEMC-SS cells treated for 24 hrs under normoxic condition followed by compound wash-out and incubated under normoxic condition for 48 hrs by alamar blue assay, IC50=2.9μM.	30199705
MDA-MB-468	Cytotoxicity assay	4 hrs	Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay, IC50=0.0062μM.	30885680
SW620	Cytotoxicity assay	4 hrs	Cytotoxicity against human SW620 cells incubated for 4 hrs under hypoxic condition followed by compound washout and measured after 5 days by SRB assay, IC50=0.052μM.	30885680
MDA-MB-468	Cytotoxicity assay	4 hrs	Cytotoxicity against human MDA-MB-468 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay, IC50=4.403μM.	30885680
SW620	Cytotoxicity assay	4 hrs	Cytotoxicity against human SW620 cells incubated for 4 hrs under aerobic condition followed by compound washout and measured after 5 days by SRB assay, IC50=20.6μM.	30885680
NCI-H460	Antiproliferative assay		Antiproliferative activity against human NCI-H460 cells in presence of N2, IC50=2μM.	30295477
NCI-H460	Antiproliferative assay		Antiproliferative activity against human NCI-H460 cells in presence of O2, IC50=25μM.	30295477
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述	Evofosfamide (TH-302)是一種選擇性低氧激活的前體藥物，靶向作用于實(shí)體瘤的hypoxic區(qū)域，IC50為19 nM，在缺氧條件下比在有氧條件下細(xì)胞毒性增強(qiáng)270倍，細(xì)胞色素P450代謝穩(wěn)定。

體外研究(In Vitro)
體外研究活性	TH-302是低氧激活的前體藥物，目前處于臨床評測階段。在含氧情況下，TH-302作用于橢圓形細(xì)胞比作用于單分子層細(xì)胞效果強(qiáng)很多。^[2] 在有氧情況下，TH-302是非常有效的，且在肝臟微粒體中很穩(wěn)定。在N₂環(huán)境下，TH-302作用于人類肺癌H460細(xì)胞和人類結(jié)腸癌HT29細(xì)胞，具有高毒性。 TH-302抑制H460細(xì)胞和HT29細(xì)胞，IC90分別為0.1和0.2 μM。^[1] TH-302作用于多發(fā)性骨髓瘤具有低氧選擇性和劑量依賴性。在低氧條件下，TH-302誘導(dǎo)細(xì)胞周期停在G0/G1 期。通過下調(diào)cyclin D1/2/3, CDK4/6, p21cip-1, p27kip-1, 和 pRb表達(dá)來調(diào)節(jié)TH-302作用于細(xì)胞周期的影響,而CDK2表達(dá)對此沒有作用效果。在低氧條件下，TH-302作用于人類和鼠多發(fā)性骨髓瘤細(xì)胞，誘導(dǎo)細(xì)胞凋亡，這種作用存在劑量依賴性。通過下調(diào)抗凋亡蛋白BCL-2和BCL-xL, 還有上調(diào)裂開的凋亡前體蛋白caspase-3,-8,和-9，及ＰＡＲＰ的表達(dá)來調(diào)節(jié)TH-302激活的凋亡。與低氧環(huán)境下特殊的毒性相比，在含氧正常的環(huán)境下或者高氧環(huán)境下，TH-302 顯示低毒性。^[3]
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	人類H460或HT29細(xì)胞
	濃度	0.01 -1 μM
	孵育時間	2小時
	方法	指數(shù)生長的人類H460或HT29細(xì)胞按每孔3×10⁵個細(xì)胞接種在60 mm有缺口的玻璃板上，在含10%FBS的RPMI培養(yǎng)基上生長2天。實(shí)驗(yàn)開始第一天,已知濃度TH-302溶液準(zhǔn)備在完全培養(yǎng)基中，玻璃板上每孔加入2 mL溶液。玻璃板置于厭氧培養(yǎng)室或標(biāo)準(zhǔn)組織培養(yǎng)孵育器。在厭氧培養(yǎng)室中充滿厭氧氣體混合物(90% N₂/5% CO₂/5% H₂)，形成低氧環(huán)境。細(xì)胞和TH-302在37^oC下溫育2小時。處理到最后，移除板，用PBS沖洗，然后用胰蛋白酶-EDTA使胰蛋白酶化，在37^oC下進(jìn)行5分鐘。分離的細(xì)胞用培養(yǎng)基和血清中和，然后在100g轉(zhuǎn)速下旋轉(zhuǎn)5分鐘。細(xì)胞按1×10⁶個細(xì)胞/mL再懸浮，然后稀釋10倍。測定每組溶液的確切濃度。已知數(shù)目的細(xì)胞在第9天和第13天接種和置于孵育器中。菌落混合，用95%乙醇和0.25%結(jié)晶紫染色。計(jì)數(shù)超過50個細(xì)胞的菌落，測定存活率。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	實(shí)驗(yàn)移植第25天，TH302抑制腫瘤生長，抑制率達(dá)41% ，但是TH302聯(lián)用抑制腫瘤生長，抑制率達(dá) 96%。^[1]TH-302按 6.25, 12.5, 25, 或50 mg/kg劑量腹腔注射到H460 NSCLC移植模型，每天處理一次，每周處理5次，持續(xù)2周，在第22天，腫瘤生長抑制率分別為43%, 51%, 75%,和 89%。TH-302 按100 mg/kg劑量作用于血細(xì)胞，處理后3天，血細(xì)胞下降，但是在處理后7天完全恢復(fù)。TH-302誘導(dǎo)細(xì)胞死亡，依賴于氧濃度，當(dāng)作用于攜帶腫瘤的鼠在低氧濃度環(huán)境下，則毒性最高。TH-302作用于呼吸氧氣需10% O₂的動物，抑制腫瘤生長明顯低于呼吸需95% O₂的動物。TH-302處理后48小時, pimonidazole陽性區(qū)明顯降低(對照組為6.3±1.2%，TH-302實(shí)驗(yàn)組為1.8±1.1%)。 ^[4]
動物實(shí)驗(yàn)	Animal Models	雌性NCI SCID鼠
	Dosages	50 mg/kg
	Administration	腹腔注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02020226	Unknown status	Solid Tumors	Threshold Pharmaceuticals	November 2013	Phase 1
NCT01833546	Completed	Solid Tumor\|Pancreatic Cancer	Merck KGaA Darmstadt Germany\|Threshold Pharmaceuticals	April 18 2013	Phase 1

參考文獻(xiàn)
[1] Duan JX, et al. J Med Chem, 2008, 51(8), 2412-2420. [2] Meng F, et al. Mol Cancer Ther, 2012, 11(3), 740-751. [3] Hu J, et al. Blood, 2010, 116(9), 1524-1527. [4] Sun JD, et al. Clin Cancer Res, 2012, 18(3), 758-770. + 展開

參考文獻(xiàn)

[1] Duan JX, et al. J Med Chem, 2008, 51(8), 2412-2420.
[2] Meng F, et al. Mol Cancer Ther, 2012, 11(3), 740-751.
[3] Hu J, et al. Blood, 2010, 116(9), 1524-1527.

[4] Sun JD, et al. Clin Cancer Res, 2012, 18(3), 758-770.

+ 展開

化學(xué)信息&溶解度

分子量	449.04	分子式	C₉H₁₆Br₂N₅O₄P
CAS號	918633-87-1	SDF	Download Evofosfamide (TH-302) SDF
Smiles	CN1C(=CN=C1[N+](=O)[O-])COP(=O)(NCCBr)NCCBr
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 90 mg/mL ( (200.42 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 90 mg/mL (200.42 mM)

Water : 10 mg/mL (22.26 mM)

DMSO : 90 mg/mL ( (200.42 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 90 mg/mL (200.42 mM)

Water : 10 mg/mL (22.26 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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